Psychostimulants Overview
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Psychostimulants Overview

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Questions and Answers

What is the primary mechanism of action (MOA) of psychostimulants?

  • Increase serotonin synthesis
  • Stimulate GABA receptors
  • Promote release of NE, DA, and 5-HT (correct)
  • Block acetylcholine receptors

    • Which of the following is a clinical indication for psychostimulants?

  • Generalized anxiety disorder
  • Moderate to severe ADHD (correct)
  • Bipolar disorder
  • Major depressive disorder

    • What is a common adverse drug reaction (ADR) associated with psychostimulant use?

  • Weight gain
  • Insomnia (correct)
  • Sedation
  • Hyperglycemia

    • Which dosing option best represents the range for Vyvanse® (lisdexamfetamine)?

    <p>30-70 mg</p> Signup and view all the answers

    Which drug interaction is a concern for atomoxetine?

    <p>Decreased metabolism by MAO inhibitors</p> Signup and view all the answers

    What is the primary mechanism of action of Atomoxetine?

    <p>Stimulates alpha-2 receptors in the brain</p> Signup and view all the answers

    Which condition is NOT indicated for the use of Atomoxetine?

    <p>Excessive daytime sleepiness</p> Signup and view all the answers

    Which of the following is NOT a common adverse drug reaction associated with Atomoxetine?

    <p>Hypertension</p> Signup and view all the answers

    What is the recommended action regarding dosage adjustment for patients with renal impairment when taking Atomoxetine?

    <p>No dose adjustment needed</p> Signup and view all the answers

    Atomoxetine has significant interactions with which of the following substances?

    <p>MAO inhibitors</p> Signup and view all the answers

    Which of the following describes the half-life of Atomoxetine in poor metabolizers of CYP2D6?

    <p>Up to $24$ hours</p> Signup and view all the answers

    Atomoxetine should be gradually withdrawn to avoid which of the following issues?

    <p>Rebound hypertension</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction that can occur with Atomoxetine use?

    <p>Elevated liver enzymes</p> Signup and view all the answers

    What is the primary mechanism of action of tricyclic antidepressants (TCA)?

    <p>Block serotonin and norepinephrine reuptake</p> Signup and view all the answers

    Which of the following is NOT a contraindication for using stimulants?

    <p>Severe anxiety disorders</p> Signup and view all the answers

    What is a potential adverse drug reaction associated with the use of tricyclic antidepressants?

    <p>Weight gain</p> Signup and view all the answers

    What is the proper management for hypertension in cases of amphetamine overdose?

    <p>Use IV phentolamine</p> Signup and view all the answers

    Which of the following interactions requires a washout period of 14 days after using MAOIs?

    <p>Stimulants</p> Signup and view all the answers

    What is the main use of Bupropion (Wellbutrin)?

    <p>Antidepressant and smoking cessation</p> Signup and view all the answers

    When managing agitation due to stimulant therapy, which medication is preferably administered?

    <p>IV diazepam</p> Signup and view all the answers

    What effect does L-lysine have during the metabolism of certain drugs?

    <p>Release of active drug, d-amphetamine</p> Signup and view all the answers

    Which strategy is recommended for managing insomnia caused by stimulant medications?

    <p>Consider melatonin at bedtime</p> Signup and view all the answers

    Which cardiovascular risk is associated with the use of certain stimulants?

    <p>Increased blood pressure</p> Signup and view all the answers

    What is the mechanism of action (MOA) for amphetamine+dextroamphetamine?

    <p>Stimulates dopamine release</p> Signup and view all the answers

    Which of the following drugs is classified as a non-CII stimulant for ADHD?

    <p>Atomoxetine HCl</p> Signup and view all the answers

    What is a common adverse drug reaction (ADR) associated with tricyclic antidepressants (TCAs)?

    <p>Hypotension</p> Signup and view all the answers

    Which of the following medications has a black box warning (BBW) related to suicidal thoughts in children and adolescents?

    <p>Atomoxetine HCl</p> Signup and view all the answers

    Methylphenidate is available in which of the following dosage forms?

    <p>Oral osmotic controlled release</p> Signup and view all the answers

    What type of drug interactions should be considered with MAO inhibitors?

    <p>Interactions leading to serotonin syndrome</p> Signup and view all the answers

    Which mechanism of action is observed in bupropion HCL?

    <p>Inhibits dopamine reuptake</p> Signup and view all the answers

    Which of the following drugs is used as an alpha-2 agonist for ADHD?

    <p>Clonidine HCl</p> Signup and view all the answers

    What type of stimulant is Modafinil classified as?

    <p>CIV stimulant</p> Signup and view all the answers

    Which of the following medications does NOT belong to the stimulant class?

    <p>Atomoxetine HCl</p> Signup and view all the answers

    What is the mechanism of action for Methylphenidate?

    <p>Dopamine and norepinephrine reuptake inhibitor</p> Signup and view all the answers

    Which condition is Modafinil primarily indicated for?

    <p>Excessive sleepiness associated with narcolepsy</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction of Armodafinil?

    <p>Dizziness</p> Signup and view all the answers

    What contraindication is associated with using Armodafinil?

    <p>Severe hepatic impairment</p> Signup and view all the answers

    Which of the following conditions can Modafinil be used off-label to treat?

    <p>ADHD</p> Signup and view all the answers

    Which side effect is commonly associated with the use of Dopamine and Norepinephrine Reuptake Inhibitors (DNRIs)?

    <p>Increased blood pressure and heart rate</p> Signup and view all the answers

    How does Clonidine affect memory?

    <p>Causes memory loss</p> Signup and view all the answers

    Which medication requires a REMS program due to its potential for illicit use?

    <p>Modafinil</p> Signup and view all the answers

    Which drug interaction should be avoided with DNRIs?

    <p>Monoamine oxidase inhibitors (MAOIs)</p> Signup and view all the answers

    What is a potential adverse effect of Modafinil?

    <p>QT prolongation</p> Signup and view all the answers

    What is the primary mechanism of action of allopurinol in relation to inflammatory diseases?

    <p>Enhances adenosine levels, thus decreasing inflammation</p> Signup and view all the answers

    Which drug interaction is most likely to affect the levels of corticosteroids used in the management of inflammatory bowel disease?

    <p>Phenytoin, which can decrease corticosteroids efficacy</p> Signup and view all the answers

    How is azathioprine metabolized in the body, and what is its dosing consideration?

    <p>Requires dose adjustment in renal dysfunction due to renal excretion</p> Signup and view all the answers

    Why is allopurinol considered a category D drug in pregnancy?

    <p>It is associated with teratogenic effects and should be avoided</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction associated with corticosteroids used in IBD management?

    <p>Mood changes and increased appetite</p> Signup and view all the answers

    What is the primary mechanism of action of purine analogs used in the treatment of IBD?

    <p>Suppress purine nucleotide metabolism and reduce DNA synthesis</p> Signup and view all the answers

    What is a significant drug interaction concern when using Azathioprine?

    <p>Increased risk of leukopenia with allopurinol</p> Signup and view all the answers

    What is a key consideration in the metabolism of Azathioprine for patients with absent TPMT?

    <p>Increased risk of myelosuppression</p> Signup and view all the answers

    Which dietary modification is recommended for patients treated with corticosteroids?

    <p>High-protein and potassium-enriched diet</p> Signup and view all the answers

    What is a common adverse drug reaction of corticosteroid use if administered for longer than 2 weeks?

    <p>Adrenal suppression</p> Signup and view all the answers

    Which of the following conditions can Azathioprine be used to prevent, aside from IBD?

    <p>Transplant rejection</p> Signup and view all the answers

    Which corticosteroid side effect may occur as a result of impaired wound healing?

    <p>Osteoporosis</p> Signup and view all the answers

    How does the metabolism of Azathioprine differ based on TPMT enzyme activity?

    <p>Slow metabolizers are at risk for increased toxicity</p> Signup and view all the answers

    What is one of the mechanisms of action of IBD agents like mesalamine?

    <p>Inhibition of inflammatory cytokines</p> Signup and view all the answers

    Which drug interaction is a concern when using sulfasalazine?

    <p>Decreased effect of digoxin</p> Signup and view all the answers

    What is a recommended dosage adjustment for managing IBD with corticosteroids during pregnancy?

    <p>Assess risk vs benefit regularly</p> Signup and view all the answers

    What is a common adverse drug reaction associated with the use of corticosteroids like prednisone?

    <p>Increased appetite</p> Signup and view all the answers

    Which medication is considered best tolerated among the IBD agents listed?

    <p>Balsalazide</p> Signup and view all the answers

    What is an important aspect of monitoring while using balsalazide as an IBD agent?

    <p>Testing renal and hepatic function</p> Signup and view all the answers

    What adverse drug reaction may occur specifically with sulfasalazine in certain patients?

    <p>Myalgia and alopecia</p> Signup and view all the answers

    Which formulation of mesalamine is designed for delivery to the rectum?

    <p>Rowasa®</p> Signup and view all the answers

    Budesonide's first-pass metabolism primarily affects which aspect of its use?

    <p>Reduced overall side effects</p> Signup and view all the answers

    Which of the following medications can lower the bioavailability of digoxin?

    <p>Sulfasalazine</p> Signup and view all the answers

    What is the primary mechanism of action of TNF inhibitors used in IBD treatment?

    <p>Inhibition of TNF activity and cytokine release</p> Signup and view all the answers

    Which of the following drugs should not be combined with CsA due to nephrotoxic risks?

    <p>Cimetidine</p> Signup and view all the answers

    Which adverse reaction is most commonly associated with long-term use of corticosteroids in IBD management?

    <p>Hypertension</p> Signup and view all the answers

    What should be monitored regularly in patients undergoing treatment with CsA?

    <p>Blood pressure and renal function</p> Signup and view all the answers

    Which condition can increase the risk of developing antibodies in patients receiving monoclonal antibody therapy?

    <p>Latent tuberculosis</p> Signup and view all the answers

    Which cytokine is primarily increased by TNF activation within the inflammatory response?

    <p>IL-1</p> Signup and view all the answers

    When treating IBD in pregnant women, which factor should clinicians consider?

    <p>The potential impact of uncontrolled disease</p> Signup and view all the answers

    What is a common adverse drug reaction associated with the use of Infliximab in treating IBD?

    <p>Increased risk of infections</p> Signup and view all the answers

    Which of the following drugs is noted for its potential hepatotoxicity when used in IBD management?

    <p>Azathioprine</p> Signup and view all the answers

    Which of the following is a common adverse reaction to corticosteroids used in IBD management?

    <p>Weight gain</p> Signup and view all the answers

    What is the primary mechanism of action of Ustekinumab in treating IBD?

    <p>Inhibition of IL-12 and IL-23 expression</p> Signup and view all the answers

    Which drug interaction is a significant concern when prescribing Tofacitinib?

    <p>Potential interactions with drugs affecting CYP 3A4 enzymes</p> Signup and view all the answers

    What is the effect of slow metabolizers on the use of purine analogs in IBD treatment?

    <p>Higher likelihood of adverse effects</p> Signup and view all the answers

    What is a concern regarding the use of corticosteroids like prednisone in IBD patients?

    <p>Limited duration of use due to side effects</p> Signup and view all the answers

    Which statement accurately reflects the use of Ozanimod in managing MS and ulcerative colitis?

    <p>It blocks lymphocytes' ability to leave lymph nodes.</p> Signup and view all the answers

    What unique risk is associated with the use of Risankizumab for treating plaque psoriasis?

    <p>Higher chances of developing infections</p> Signup and view all the answers

    What is a primary consideration when using live vaccines in patients undergoing treatment for IBD?

    <p>Patients should never receive live vaccines.</p> Signup and view all the answers

    What is the dosing schedule for Ustekinumab in patients with inflammation?

    <p>300 mg IV on 0, 2, 6 weeks, then every 8 weeks</p> Signup and view all the answers

    What type of drug is Tofacitinib, and what is its primary indication?

    <p>Janus kinase inhibitor for rheumatoid arthritis</p> Signup and view all the answers

    Which of the following describes a common adverse drug reaction of Ozanimod?

    <p>Macular edema</p> Signup and view all the answers

    Which of the following is an adverse drug reaction associated with glucocorticosteroids related to hyperfunction of glands?

    <p>Cushing syndrome</p> Signup and view all the answers

    What condition is a result of adrenal gland hypofunction linked to glucocorticosteroids?

    <p>Addison's disease</p> Signup and view all the answers

    Which hormone is secreted by the anterior pituitary as a result of hypothalamic stimulation by GHRH?

    <p>GH</p> Signup and view all the answers

    Which hormone acts through JAK/STAT receptors rather than G protein coupled receptors in the pituitary?

    <p>Prolactin</p> Signup and view all the answers

    Which of the following conditions is linked to hyperfunction of the pituitary gland due to glucocorticosteroid use?

    <p>Acromegaly</p> Signup and view all the answers

    Which target organ is primarily stimulated by ACTH released from the anterior pituitary?

    <p>Adrenal cortex</p> Signup and view all the answers

    Which condition is characterized by a decrease in aldosterone secretion due to adrenal gland issues?

    <p>Hypoaldosteronism</p> Signup and view all the answers

    What is the function of somatostatin regarding the anterior pituitary's hormone release?

    <p>Inhibits PRL and GH release</p> Signup and view all the answers

    What is one of the primary uses of Mifepristone?

    <p>Termination of early pregnancy</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction (ADR) associated with Mifepristone?

    <p>Diarrhea</p> Signup and view all the answers

    What is the mechanism of action of Cyproheptadine?

    <p>Decreases ACTH release</p> Signup and view all the answers

    In which condition is aldosterone usually elevated?

    <p>Primary aldosteronism</p> Signup and view all the answers

    What should be considered when using Cyproheptadine?

    <p>It may interact with diuretics</p> Signup and view all the answers

    Which type of hormone is derived from cholesterol?

    <p>Steroid hormones</p> Signup and view all the answers

    What is the mechanism of action of GH antagonists?

    <p>Bind to GH receptors in liver</p> Signup and view all the answers

    Which drug is a somatostatin analogue used to inhibit GH?

    <p>Octreotide</p> Signup and view all the answers

    Which hormone is primarily associated with acromegaly treatment?

    <p>Growth hormone (GH)</p> Signup and view all the answers

    What is a common adverse reaction associated with somatostatin analogues?

    <p>Hypoglycemia</p> Signup and view all the answers

    Which condition requires glucocorticoids among the treatment options?

    <p>Addison's disease</p> Signup and view all the answers

    Dopamine agonists are used to reduce which hormone levels?

    <p>Growth hormone (GH)</p> Signup and view all the answers

    Which of the following hormones are classified as polypeptide/protein hormones?

    <p>Oxytocin</p> Signup and view all the answers

    What therapeutic goal is pursued in the treatment of acromegaly?

    <p>Decrease IGF and GH levels</p> Signup and view all the answers

    Which drug is known for its hepatotoxicity as an adverse drug reaction?

    <p>Pegvisomant</p> Signup and view all the answers

    What are the possible etiologies of growth failure due to adrenal disorders?

    <p>Congenital, Acquired, Idiopathic</p> Signup and view all the answers

    Which hormone mainly mediates the growth-promoting effects of growth hormone (GH)?

    <p>IGF-1</p> Signup and view all the answers

    What is a common adverse reaction associated with recombinant human growth factor (rhGH) administration?

    <p>Intracranial hypertension</p> Signup and view all the answers

    What is the primary function of glucocorticoids such as cortisol?

    <p>Aids in protein, carbohydrate, and fat metabolism</p> Signup and view all the answers

    Which mineralocorticoid primarily maintains electrolyte and volume homeostasis?

    <p>Aldosterone</p> Signup and view all the answers

    What is the role of glucocorticoids during periods of stress?

    <p>Increase glucocorticoid levels</p> Signup and view all the answers

    What is the primary route of metabolism for glucocorticoids?

    <p>Glucuronidation in the liver</p> Signup and view all the answers

    What potential complication can arise from prolonged use of glucocorticoids?

    <p>Systemic adverse reactions</p> Signup and view all the answers

    Which of the following drugs may inhibit the effect of growth hormone?

    <p>Glucocorticoids</p> Signup and view all the answers

    What should glucocorticoids be administered with to avoid gastrointestinal problems?

    <p>With meals</p> Signup and view all the answers

    What is a consequence of using oral glucocorticoids for more than 2 weeks?

    <p>Systemic adverse drug reactions</p> Signup and view all the answers

    Why is tapering necessary before discontinuing glucocorticoids?

    <p>To prevent rebound symptoms and adrenal suppression</p> Signup and view all the answers

    Which of the following is NOT a commonly monitored parameter during glucocorticoid therapy?

    <p>Liver enzymes</p> Signup and view all the answers

    What kind of imbalance does glucocorticoid use create that impacts bone health?

    <p>Altered osteoclast and osteoblast balance</p> Signup and view all the answers

    What is a common adverse drug reaction associated with glucocorticoid therapy relating to infection?

    <p>Increased risk of infection</p> Signup and view all the answers

    Which metabolic change is NOT typically caused by glucocorticoids?

    <p>Decreased lipolysis</p> Signup and view all the answers

    Which of the following is a behavioral side effect associated with glucocorticoid use?

    <p>Psychosis</p> Signup and view all the answers

    What is a primary effect of glucocorticoids on muscle tissue?

    <p>Muscle catabolism</p> Signup and view all the answers

    Which effect is associated with glucocorticoid-induced hypertension?

    <p>Increased sodium and water retention</p> Signup and view all the answers

    What is a common gastrointestinal complication associated with glucocorticoid use?

    <p>Exacerbation of peptic ulcers</p> Signup and view all the answers

    What are potential adverse drug reactions (ADRs) associated with muscle relaxants?

    <p>Tolerance and dependence</p> Signup and view all the answers

    Which of the following describes the mechanism of action of dantrolene?

    <p>Blockage of RyR1 calcium channels</p> Signup and view all the answers

    Which of the following interactions is particularly concerning when using tizanidine?

    <p>Ciprofloxacin</p> Signup and view all the answers

    What should be avoided while using CNS depressants?

    <p>Alcohol and benzodiazepines</p> Signup and view all the answers

    What is the primary clinical use of dantrolene?

    <p>Malignant hyperthermia</p> Signup and view all the answers

    What is the mechanism of action (MOA) of neuromuscular blocking drugs?

    <p>They block transmission at the neuromuscular end plate.</p> Signup and view all the answers

    Which drug is classified as a depolarizing neuromuscular agent?

    <p>Succinylcholine</p> Signup and view all the answers

    Which of the following is an adverse drug reaction (ADR) associated with centrally acting spasmolytic drugs?

    <p>Sedation and dizziness</p> Signup and view all the answers

    What counseling point is important when using muscle relaxants?

    <p>Avoid activities requiring mental alertness during use.</p> Signup and view all the answers

    Which spasmolytic drug is known for its central action?

    <p>Carisoprodol</p> Signup and view all the answers

    Which drug is better suited for patients with ALS among non-depolarizing neuromuscular agents?

    <p>Cisatracurium</p> Signup and view all the answers

    What is a characteristic feature of Cisatracurium?

    <p>It undergoes spontaneous degradation at physiological pH.</p> Signup and view all the answers

    Which centrally acting spasmolytic drug is also used as an anticonvulsant?

    <p>Gabapentin</p> Signup and view all the answers

    What is the primary effect of spasmolytics?

    <p>Treat chronic pain and reduce spasticity</p> Signup and view all the answers

    How do neuromuscular blockers like D-tubocurarine exert their effects?

    <p>As a competitive antagonist of nAChR</p> Signup and view all the answers

    What occurs immediately after the binding of ACH to nAChR?

    <p>Opening of the channel causing Na+ influx</p> Signup and view all the answers

    What is the mechanism of action (MOA) of succinylcholine?

    <p>Agonism of nAChR leading to depolarization</p> Signup and view all the answers

    Which of the following is a potential adverse drug reaction (ADR) of succinylcholine?

    <p>Arrhythmias</p> Signup and view all the answers

    What differentiates Mivacurium from D-tubocurarine?

    <p>Mivacurium is metabolized by plasma cholinesterase</p> Signup and view all the answers

    What characterizes the effects of D-tubocurarine at the neuromuscular junction?

    <p>Preventing ACH binding to nAChR</p> Signup and view all the answers

    What is a key feature of the end plate potential that indicates strong depolarization?

    <p>Causing an action potential to propagate</p> Signup and view all the answers

    What is a primary characteristic of persistent muscle paralysis induced by depolarizing agents?

    <p>Transient contraction followed by paralysis</p> Signup and view all the answers

    Which agent is best known for causing muscle paralysis during surgery with a short duration of action?

    <p>Succinylcholine</p> Signup and view all the answers

    Which type of muscle relaxant is more commonly used in an ICU setting?

    <p>Rocuronium</p> Signup and view all the answers

    What is the primary mechanism through which baclofen operates?

    <p>GABAB receptor agonism</p> Signup and view all the answers

    Which muscle relaxant specifically acts on the sarcoplasmic reticulum of skeletal muscle?

    <p>Dantrolene</p> Signup and view all the answers

    Which of the following classes of drugs is known for causing sedation as a common adverse drug reaction?

    <p>Tizanidine</p> Signup and view all the answers

    What is a common effect of spasticity resulting from central nervous system damage?

    <p>Muscle stiffness and spasms</p> Signup and view all the answers

    Which muscle relaxant acts by inhibiting the muscle stretch reflex in the spinal cord?

    <p>Cyclobenzaprine</p> Signup and view all the answers

    Which drug's primary mechanism of action involves GABAergic transmission enhancement?

    <p>Diazepam</p> Signup and view all the answers

    What common adverse drug reaction is associated with diazepam?

    <p>Dependence</p> Signup and view all the answers

    Which of the following has an α2 agonist mechanism of action for spasmolytic effects?

    <p>Tizanidine</p> Signup and view all the answers

    What is a mechanism related to spasticity due to central nervous system damage?

    <p>Hyperactivity of α motor neurons</p> Signup and view all the answers

    What is the duration of action of Rocuronium?

    <p>20-35 minutes</p> Signup and view all the answers

    Which non-depolarizing relaxant has the highest potency compared to D-tubocurarine?

    <p>Vecuronium</p> Signup and view all the answers

    What is a key characteristic of Cisatracurium's metabolism?

    <p>Hofmann elimination</p> Signup and view all the answers

    Which of the following drugs has an onset time of 1-2 minutes?

    <p>Rocuronium</p> Signup and view all the answers

    What adverse drug reaction is less likely to occur with D-tubocurarine compared to other non-depolarizing relaxants?

    <p>Histamine release</p> Signup and view all the answers

    Which non-depolarizing relaxant may improve mortality in patients with moderate to severe acute respiratory syndrome?

    <p>Cisatracurium</p> Signup and view all the answers

    What is the primary route of administration for these polar drugs?

    <p>Iv only</p> Signup and view all the answers

    Which non-depolarizing relaxant has a longer duration of action due to renal elimination?

    <p>Vecuronium</p> Signup and view all the answers

    Which metabolite percentage is typical for the drugs being discussed?

    <p>40-80%</p> Signup and view all the answers

    What type of effect does Cisatracurium have regarding histamine release?

    <p>Decreases histamine release</p> Signup and view all the answers

    What is a significant concern when combining tizanidine with ciprofloxacin?

    <p>Increased sedation and confusion</p> Signup and view all the answers

    Which of the following is NOT a common adverse drug reaction (ADR) associated with dantrolene?

    <p>Headache</p> Signup and view all the answers

    What is the primary mechanism of action (MOA) of dantrolene?

    <p>Blocking RyR1 calcium channels</p> Signup and view all the answers

    What are the potential risks associated with the use of tizanidine and CNS depressants?

    <p>Additive sedation and confusion</p> Signup and view all the answers

    What drug is used to manage malignant hyperthermia during anesthesia?

    <p>Dantrolene</p> Signup and view all the answers

    What is a major use of neuromuscular blocking drugs during surgical procedures?

    <p>Producing muscle paralysis</p> Signup and view all the answers

    Which drug is classified as a non-depolarizing neuromuscular agent?

    <p>Cisatracurium</p> Signup and view all the answers

    Which centrally acting spasmolytic drug is known for its mechanism of action that involves GABA-B receptors?

    <p>Baclofen</p> Signup and view all the answers

    What is a potential adverse drug reaction (ADR) associated with the use of muscle relaxants?

    <p>Drowsiness</p> Signup and view all the answers

    Which drug can be useful as a spasmolytic agent besides baclofen?

    <p>Gabapentin</p> Signup and view all the answers

    What is a key counseling point for patients using spasmolytic drugs?

    <p>Be cautious with driving</p> Signup and view all the answers

    Which of the following represents important characteristics of Cisatracurium?

    <p>It's safe for patients with renal impairment</p> Signup and view all the answers

    Which muscle relaxant is not classified under centrally acting spasmolytics?

    <p>Cisatracurium</p> Signup and view all the answers

    What is the primary concern associated with prolonged use of neuromuscular blockers in an ICU setting?

    <p>Muscle paralysis due to metabolite accumulation</p> Signup and view all the answers

    Which drug is associated with acting on the GABAB receptors to inhibit motor neurons?

    <p>Baclofen</p> Signup and view all the answers

    Which statement about spasmolytics is true?

    <p>They are used to reduce spasticity in various painful conditions.</p> Signup and view all the answers

    What mechanism of action does tizanidine primarily utilize?

    <p>Alpha-2 agonism in the spinal cord</p> Signup and view all the answers

    Which medication primarily works by acting on the sarcoplasmic reticulum in skeletal muscle?

    <p>Dantrolene</p> Signup and view all the answers

    What occurs at the motor end plate when acetylcholine binds to nAChR?

    <p>The channel opens allowing Na+ and K+ movement.</p> Signup and view all the answers

    Which of the following drugs is likely to cause sedation and muscle weakness as adverse effects?

    <p>Tizanidine</p> Signup and view all the answers

    What is the mechanism of action of succinylcholine?

    <p>It is an agonist of nAChR, causing initial depolarization.</p> Signup and view all the answers

    Which drug is known for causing prolonged flaccid paralysis?

    <p>Succinylcholine</p> Signup and view all the answers

    What is the primary therapeutic effect of baclofen?

    <p>Decrease motor output in the spinal cord</p> Signup and view all the answers

    What type of muscle activity does spasticity involve?

    <p>Increased tonic stretch reflexes and muscle spasms</p> Signup and view all the answers

    What is a common adverse reaction associated with D-tubocurarine?

    <p>Apnea</p> Signup and view all the answers

    Which of the following drugs has an anti-muscarinic effect?

    <p>Cyclobenzaprine</p> Signup and view all the answers

    Why might mivacurium's effects be short-lived?

    <p>It undergoes hydrolysis by plasma cholinesterase.</p> Signup and view all the answers

    What is the onset time for succinylcholine?

    <p>1-1.5 minutes</p> Signup and view all the answers

    Which compound's action is predominantly attributed to enhancing GABAergic transmission?

    <p>Diazepam</p> Signup and view all the answers

    What underlying issue causes spasticity in various neurological conditions?

    <p>Hyperactivity of alpha motor neurons</p> Signup and view all the answers

    What is the primary role of acetylcholinesterase at the neuromuscular junction?

    <p>To remove acetylcholine from the synaptic cleft.</p> Signup and view all the answers

    What does D-tubocurarine do at the neuromuscular junction?

    <p>Blocks the action of acetylcholine.</p> Signup and view all the answers

    Which condition is D-tubocurarine mainly used to treat?

    <p>Flaccid paralysis during surgery.</p> Signup and view all the answers

    What is the duration of action for Rocuronium (Zemuron®)?

    <p>20-35 minutes</p> Signup and view all the answers

    Which drug is metabolized via Hofmann elimination?

    <p>Cisatracurium</p> Signup and view all the answers

    What is the onset time for Vecuronium (Norcuron®)?

    <p>2-4 minutes</p> Signup and view all the answers

    Which drug has a potency 6 times that of D-tubocurarine?

    <p>Vecuronium</p> Signup and view all the answers

    What common adverse drug reaction is associated with Cisatracurium?

    <p>Flushing</p> Signup and view all the answers

    What is the primary route of elimination for Vecuronium?

    <p>Renal and hepatic elimination</p> Signup and view all the answers

    Which of the following drugs tends to have a longer duration of action due to renal elimination?

    <p>D-tubocurarine</p> Signup and view all the answers

    Which drug has a duration of action ranging from 60-90 minutes?

    <p>Vecuronium</p> Signup and view all the answers

    Which antimuscarinic effect is observed with tubocurarine?

    <p>Decreased salivation</p> Signup and view all the answers

    Which drug has a slower onset time of 1-2 minutes?

    <p>Rocuronium</p> Signup and view all the answers

    Which of the following symptoms is commonly associated with hyperprolactinemia in females?

    <p>Galactorrhea</p> Signup and view all the answers

    What is a common adverse effect of Bromocriptine treatment?

    <p>Dizziness</p> Signup and view all the answers

    Which medication is noted for being more effective in decreasing prolactin levels and tumor size?

    <p>Cabergoline</p> Signup and view all the answers

    What condition can spironolactone effectively treat?

    <p>Galactorrhea</p> Signup and view all the answers

    What are the symptoms of Addison's disease?

    <p>Fatigue, skin hyperpigmentation, muscle weakness</p> Signup and view all the answers

    What is a potential adverse drug reaction (ADR) associated with drugs used to treat acromegaly?

    <p>Hyperglycemia</p> Signup and view all the answers

    Which hormone is primarily related to acromegaly and has a significant connection with dopamine?

    <p>Growth Hormone</p> Signup and view all the answers

    Which drug is commonly used to treat Cushing syndrome and has notable drug interactions?

    <p>Spironolactone</p> Signup and view all the answers

    What is a common method of administration for drugs used to treat Addison's disease?

    <p>Oral formulation</p> Signup and view all the answers

    Which of the following hormones is released by the hypothalamus and regulates the secretion of growth hormone?

    <p>Growth Hormone Releasing Hormone</p> Signup and view all the answers

    What is the primary mechanism of action (MOA) for somatostatin analogues used in the treatment of acromegaly?

    <p>Inhibition of growth hormone release</p> Signup and view all the answers

    Which medication is specifically indicated for managing hyperprolactinemia?

    <p>Bromocriptine</p> Signup and view all the answers

    Which drug class would be indicated for the treatment of conditions related to aldosterone antagonism?

    <p>Potassium-sparing diuretics</p> Signup and view all the answers

    Which condition is caused by hyperfunction of the adrenal glands?

    <p>Cushing syndrome</p> Signup and view all the answers

    What is a potential consequence of adrenal hypofunction?

    <p>Short stature</p> Signup and view all the answers

    What is a major consequence of suppressing the local immune response against H. pylori?

    <p>Activation of H. pylori</p> Signup and view all the answers

    What effect do glucocorticoids have on bodily fat distribution?

    <p>They lead to fat accumulation in specific areas.</p> Signup and view all the answers

    Which hormone is primarily affected by somatostatin?

    <p>GH</p> Signup and view all the answers

    Which of the following hormones is released due to Corticotropin-Releasing Hormone (CRH)?

    <p>ACTH</p> Signup and view all the answers

    What is a recommended strategy to prevent iatrogenic Cushing syndrome?

    <p>Avoid administration routes with systemic absorption.</p> Signup and view all the answers

    Which of the following describes a possible effect of hyperfunction of the pituitary gland?

    <p>Acromegaly</p> Signup and view all the answers

    How should glucocorticoid doses be reduced after treatment to avoid withdrawal symptoms?

    <p>Gradually decrease the dose per day.</p> Signup and view all the answers

    What role do glucocorticoids play during the skeletal growth phase?

    <p>They decrease osteoblast precursors.</p> Signup and view all the answers

    What does the increased production of PRL from the pituitary typically result in?

    <p>Breast development</p> Signup and view all the answers

    Which of the following hormones is NOT released from the adrenal cortex?

    <p>Prolactin</p> Signup and view all the answers

    Which of the following statements about glucocorticoids is correct?

    <p>Synthetic glucocorticoids generally have more growth-suppressing effects.</p> Signup and view all the answers

    What is a potential metabolic change associated with iatrogenic Cushing syndrome?

    <p>Hyperglycemia</p> Signup and view all the answers

    Which endocrine issue is associated with decreased testosterone levels?

    <p>Hypogonadism</p> Signup and view all the answers

    Which of the following is NOT a recommended practice to avoid Cushing syndrome?

    <p>Continue therapy for the longest duration possible</p> Signup and view all the answers

    What outcome is likely when there is excessive production of ACTH?

    <p>Hyperfunction of the adrenal gland</p> Signup and view all the answers

    Which of the following conditions is characterized by a deficiency in cortisol production?

    <p>Addison's disease</p> Signup and view all the answers

    What is one of the effects of long-term glucocorticoid use on the eye?

    <p>Risk of glaucoma</p> Signup and view all the answers

    What is the appropriate tapering strategy for glucocorticoids?

    <p>Continue tapering until a physiologic dose is reached.</p> Signup and view all the answers

    Which hormones are derived from tyrosine or tryptophan?

    <p>Norepinephrine, Epinephrine, Melatonin, T4</p> Signup and view all the answers

    Which class of hormones consists of chains of amino acids?

    <p>Polypeptide/protein hormones</p> Signup and view all the answers

    What is the mechanism of action of GH antagonists?

    <p>Bind to GH receptors in the liver</p> Signup and view all the answers

    Which medication is a somatostatin analogue used to inhibit GH?

    <p>Octreotide</p> Signup and view all the answers

    What is a common adverse drug reaction associated with somatostatin analogues?

    <p>Gallstones</p> Signup and view all the answers

    Which condition is treated with recombinant growth factor?

    <p>Short stature</p> Signup and view all the answers

    What is the primary action of bromocriptine?

    <p>Decrease GH and PRL levels</p> Signup and view all the answers

    Which drug is used in the treatment of Addison’s disease?

    <p>Glucocorticoids</p> Signup and view all the answers

    What is a mechanism of action for somatostatin analogues?

    <p>Inhibit gastrin and insulin</p> Signup and view all the answers

    Which of the following medications is NOT indicated for treating Cushing syndrome?

    <p>Bromocriptine</p> Signup and view all the answers

    Study Notes

    Psychostimulants:

    • Used for moderate to severe attention deficit hyperactivity disorder (ADHD)
    • Improves core symptoms: inattention, impulsivity, hyperactivity
    • Can also improve other symptoms: non-compliance, impulsive aggression, social interactions, academic efficiency and accuracy, family dynamics
    • Promote release of norepinephrine (NE), dopamine (DA), and serotonin (5-HT) from nerve terminals
    • Increase catecholamine in the synaptic cleft (inhibit reuptake)
    • Inhibit the action of monoamine oxidase (MAO)
    • Absorbed through kidneys, lungs, and brain

    Psychomimetics:

    • Different from psychostimulants
    • Not specified in text

    Specific Psychostimulants:

    • Adderall XR® (amphetamine+dextroamphetamine): 10-hour half-life, 10-30mg dose
    • Desoxyn® (methamphetamine): 4-5-hour half-life, 10-25mg dose
    • Dexedrine Spansule® (dextroamphetamine SR): 7-hour half-life, 5-15mg dose
    • Dexedrine® (dextroamphetamine): 5-hour half-life, 5-14mg dose
    • Vyvanse® (lisdexamfetamine): 10-12-hour half-life, 30-70mg dose
    • Metadate CD® (methylphenidate ER): 8-hour half-life, 20-60mg dose
    • Concerta® (methylphenidate ER): 9-10-hour half-life, 18-72mg dose
    • Ritalin LA® (methylphenidate ER): 7-8-hour half-life, 10-60mg dose
    • Methylin ER® (methylphenidate ER): 6-hour half-life, 20-30mg dose
    • Focalin® (dexmethylphenidate): 4-hour half-life, 2.5-15mg dose
    • Focalin XR® (dexmethylphenidate): 8-hour half-life, 5-20mg dose
    • Daytrana® (Methylphenidate patch): 12-hour half-life, 10-30mg dose
    • Quillivant XR® (methylphenidate)--powder: 5-hour half-life, 20-60mg dose

    ### Glucocorticoids

    • Long-term use (more than 2 weeks) can cause iatrogenic Cushing's syndrome and adrenal suppression
    • Other adverse drug reactions (ADRs) include: insomnia, behavioral changes (mainly hypomania), acute peptic ulcers, protein breakdown (catabolism), hyperglycemia, impaired wound healing, immunosuppression (lower resistance to infection), osteoporosis, increased intraocular pressure, hypertension, and hypokalemia
    • Patients treated with corticosteroids should follow a high-protein and potassium-enriched diet
    • Used for relapsing inflammatory bowel disease (IBD) that required high doses of glucocorticoids, but need to taper off the dose
    • Do not stop taking glucocorticoids abruptly

    ### Purine Analogs

    • Purine analogs are antimetabolites
    • They suppress purine nucleotide metabolism and decrease DNA synthesis, thus inhibiting cell division and proliferation (inhibiting B and T cells function)
    • Although not an FDA indication for IBD, they are used in induction and maintenance during remission
    • Examples include Azathioprine (AZA) and 6-mercaptopurine (6-MP)

    ###  Metabolism of AZA and 6-MP

    • AZA and 6-MP are metabolized through three pathways:
      • Oxidative pathway: xanthine oxidase (XO) converts AZA to 6-thiouric acid (6-TU), which is inactive
      • S-methylation by thiopurine methyltransferase (TPMT) converts 6-MP to 6-methylmercaptopurine (6-MMP), which is inactive
      • Hypoxanthine-guanine phosphoribosyltransferase (HGPRT) converts 6-MP to the active nucleotide 6-thioguanine nucleotide (6-TGN)
    • AZA is metabolized to the active 6-MP by glutathione sulfhydryl
    • Half-life of AZA and 6-MP is short, while the half-life of 6-TG is longer (days), and it is concentrated in cells
    • Due to the prolonged onset of 6-TG, the therapeutic effect of AZA is observed after several weeks
    • Drugs: Azathioprine (Imuran®) and 6-mercaptopurine (Purinethol®) which is similar to AZA, but with fewer ADRs. Take on an empty stomach
    • Uses: IBD, prevention of transplant rejection, rheumatoid arthritis (RA), multiple sclerosis (MS)

    ###  TPMT and ADRs

    • Individuals with absent or slow TPMT activity are at a higher risk of myelosuppression due to increased 6-TG levels
    • Rapid metabolizers clear the drug four times faster
    • TPMT levels can be measured before starting therapy
    • Allopurinol causes leukopenia and requires a dose reduction for AZA to one-fourth or one-third (avoid use of live vaccines)

    ###  Ustekinumab and Risankizumab

    • Mode of action: interfering with the overexpression of IL-12 and IL-23, leading to decreased T cell activation and disruption of immune cells that cause inflammation
    • Drugs: Ustekinumab (Stelara®) and Risankizumab (Skyrizi®) which only targets IL-23
    • Indications: IBD, psoriasis arthritis, plaque psoriasis
    • ADRs: pneumonia, increased risk of tuberculosis, increased risk of developing cancer, infusion reaction (pre-medicate with diphenhydramine, acetaminophen, slow infusion, or use methylprednisolone)
    • Dosing: 90mg subcutaneous dose eight weeks after the initial intravenous dose, followed by every eight weeks thereafter

    ###  Tofacitinib

    • Mode of action: inhibits Janus kinase enzymes that stimulate immune cell functions
    • Drug: Tofacitinib (Xeljanz®)
    • Indications: IBD, RA (rheumatoid arthritis)
    • ADRs: elevated liver function tests (LFTs), elevated lipids, infusion reaction, infection, neutropenia
    • Drug-drug interactions (DDI): CYP3A4 and 2C19
    • Black box warning (BW): increased risk of tuberculosis, fungal, viral, and bacterial infections, increased risk of lymphoma and cancer

    ###  Ozanimod

    • Mode of action: blocks lymphocytes from emerging from lymph nodes, decreasing their availability to the central nervous system (CNS) or intestine, leading to reduced inflammation; an immune modulator
    • Drug: Ozanimod (Zeposia®)
    • Indications: relapsing forms of multiple sclerosis (MS) and ulcerative colitis
    • Black Box Warning (BBW): myocardial infarction (MI), angina, stroke, heart failure (HF), atrioventricular block, sleep apnea, monoamine oxidase (MAO) inhibitors
    • ADRs: macular edema, upper respiratory tract infection (URI), urinary tract infection (UTI), increased blood pressure (BP), slowed heart rate, orthostatic hypotension, increased infection
    • DDIs: gemfibrozil, MAO inhibitors, live vaccines, CYP2C8 inhibitors or inducers, beta-blockers (BBs), calcium channel blockers (CCBs), drugs that cause QT prolongation

    ###  Sulfasalazine

    • Can cause folate deficiency and requires folate supplementation
    • It works by decreasing inflammation, inhibiting bacterial growth, and reducing the immune response.
    • The active drug is 5-aminosalicylic acid (5-ASA)

    ###  Purine Analogs and IBD

    • Purine analogs work by inhibiting cell division and proliferation, which can cause myelosuppression in slow metabolizers.
    • They are not useful as anti-inflammatory agents.

    ###  Tumor Necrosis Factor (TNF) Blockers

    • Anti-TNF agents include Infliximab and Adalimumab
    • They can cause increased risk of infections, reactivation of latent tuberculosis, increased risk of lymphoma, and heart failure (HF).

    ###  Prednisone

    • Prescribed for IBD patients that need rapid reduction of inflammation
    • Iatrogenic Cushing's syndrome is an ADR of prednisone excess

    ###  Ustekinumab

    • Ustekinumab works as an IL-12 and IL-23 antagonist.
    • Is indicated for psoriasis, psoriatic arthritis, and Crohn's disease.

    ###  Azo compounds

    • Azo compounds are used to treat IBD, and they include:
      • Sulfasalazine (Azulfidine®, Sulfazine®)
      • Olsalazine (Dipentum®) (ADRs: watery diarrhea, abdominal pain)
      • Balsalazide (best tolerated) (Colazal® - TID, Giazo® - BID for males)

    ###  Mesalamine

    • Mesalamine is available in various formulations to target different parts of the gastrointestinal tract:
      • Pentasa® (time-release micro-granules that release 5-ASA in the small intestine, jejunum)
      • Asacol® (5-ASA is coated to dissolve at pH 7 in the distal ileum and proximal colon; interacts with digoxin, given TID)
      • Lialda® (pH-dependent resin, slow release throughout the colon)
      • Rowasa® (5-ASA enema, delivered to the rectum)
      • Canasa® (5-ASA suppositories, delivered to the rectum)

    ###  Sulfasalazine- Specific

    • Sulfasalazine is the least expensive but has the highest ADRs
    • ADRs: headaches (HA), rash, nausea (N), vomiting (V), diarrhea (D) (40% experience these), myalgia, alopecia, folate deficiency (requires 1 g/day folic acid supplementation), yellow-orange discoloration of skin and urine
    • DDIs: decreases digoxin, iron, folic acid, and para-aminobenzoic acid (PABA) drug effects; increases oral anticoagulant, methotrexate (MTX), and oral hypoglycemic effects
    • Avoid use with antacids, H2 receptor antagonists (H2RAs), and proton pump inhibitors (PPIs) due to interference with absorption
    • Pregnancy category B, but category D at term
    • Contraindications: sulfa or salicylate allergies, gastrointestinal or genitourinary obstruction

    ###  Glucocorticoids - Specific

    • Glucocorticoids inhibit the production of inflammatory cytokines (TNF-α, IL-1, and IL-8), phospholipase A, and nitric oxide synthase.
    • Drugs: prednisone, prednisolone (QD dosing), IV methylprednisolone (severe patients), hydrocortisone (enemas, foam, rectal, and suppositories), budesonide (first-pass metabolism by CYP3A4, low oral bioavailability, budesonide CR (Entocort®) releases the drug in the distal ileum and colon)

    ###  Cyclosporine

    • Cyclosporine (CSA) has two modes of action:
      • It binds to cyclophilin, forming a complex with calcineurin, which prevents nuclear factor of activated T cells (NFATc) from forming, which decreases IL-2 and T and B cell function
    • The drug is also called a calcineurin inhibitor.
    • There are two formulations of CSA:
      • Sandimmune® (low bioavailability)
      • Neoral® and Gengraf® (modified microemulsion, better bioavailability)

    ###  Cyclosporine DDI

    • Many drugs affect CSA levels.
    • CSA is metabolized by CYP3A4, so inducers or inhibitors can affect its levels.
    • Inhibitors: ketoconazole, verapamil, cimetidine, grapefruit juice, fluvoxamine (stronger than ketoconazole and CSA)
    • Inducers: rifampin, phenytoin, phenobarbital, carbamazepine, isoniazid, St. John's wort
    • Monitor: blood pressure (BP), renal function, electrolytes, complete blood count (CBC), signs of infection
    • Maintenance levels: trough or two hours after dosing

    ###  Tumor Necrosis Factor (TNF)

    • TNF is produced by innate immunity (macrophages, dendritic cells), adaptive immune system (especially Th1 cells), and non-immune cells (fibroblasts, smooth muscle cells).
    • TNF can lead to the production of multiple cytokines such as IL-1, IL-6 and increase inflammation.
    • TNF exists as soluble and membrane-bound forms.
    • TNF binds to a TNF receptor, activating NF-κB, which increases proinflammatory cytokines, T cell activation and proliferation, leukocyte migration, and apoptosis.

    ###  TNF Blockers - Specific

    • Monoclonal antibodies (mAbs) against TNF have adverse drug reactions (ADRs) that require purified protein derivative (PPD) testing for possible latent tuberculosis activation.
    • Development of antibodies to antibodies occurs in between 3%-10% of patients. This can eliminate the desired clinical response or increase the likelihood of developing acute or delayed injection reactions.
    • For mild or self-limiting ATA, prophylaxis with acetaminophen, diphenhydramine, and corticosteroids can be given.

    ###  TNF Blockers: Mechanism

    • They inhibit soluble and membrane-bound TNF, which are pro-inflammatory.
    • Inhibit T cell and macrophage function, decreasing cytokine release.

    ###  Infliximab

    • Infliximab (Remicade®)
    • ADRs: increased risk of infections, reactivation of latent tuberculosis, increased risk of hepatitis B, increased risk of lymphoma, HF, hematologic, and hepatotoxicity

    ###  Allopurinol

    • Allopurinol is a xanthine oxidase inhibitor.
    • ADRs: N/V, anemia, hepatotoxicity, rash.
    • Black Box Warning (BBW): lymphoma, leukopenia, thrombocytopenia.
    • Monitor: CBC, platelet count, liver function test.
    • Pregnancy D. It crosses the placenta, but can be used in pregnancy.
    • Dose adjustment required in renal dysfunction.

    ###  Methotrexate

    • Mode of action:
      • At low doses, it acts as a folate antagonist, inhibiting AICAR transformylase and thymidylate synthase, leading to increased AICAR, increased adenosine, and decreased IL-2, reducing inflammation.
      • At high doses, it acts as a folate antagonist inhibiting dihydrofolate reductase (DHFR), decreasing tetrahydrofolate (FH4) and dihydrofolate (FH2), inhibiting cell-mediated immune reactions, decreasing polymorphonuclear leukocytes (PMNs), and reducing inflammation.
    • Indications: treatment of Crohn's disease, autoimmune diseases (RA, psoriasis, systemic lupus erythematosus, dermatomyositis), anti-cancer, immunosuppressant
    • Distribution: 70% of the drug is absorbed and is intracellularly polyglutamated, increasing the duration of MTX action.
    • Excretion: 70% renal and 30% bile
    • Half-life: 6-9 hours, up to 24 hours in some patients. Dose adjustment required in renal dysfunction.
    • Formulations: intrathecal, IV, PO. It does not cross the blood-brain barrier (BBB).
    • Monitor: renal, liver function test, pulmonary, neurologic, and seizure activity
    • Teratogenic. Do not use in pregnancy (category X). Pregnancy should be avoided for at least 3 months in males even after discontinuing treatment.

    ###  Methotrexate ADRs

    • ADRs: myelosuppression, severe oral ulceration/stomatitis, renal, N/V, increased LFTs, pneumonitis, photosensitivity, alopecia, crystalluria at high doses (requiring hydration and alkaline urine to reduce renal toxicity)
    • During overdose or oncologic use, leucovorin (an analog of FH4) can bypass the enzyme block and replenish the folate pool
    • At doses used to treat IBD, bone marrow suppression is rarely observed. Maintaining hydration and nutrition is important, as well as taking folic acid as directed.
    • DDIs: NSAIDs prolong MTX levels; corticosteroids decrease MTX uptake (separate administration by 12 hours)

    ###  Cyclosporine

    • Mode of action: it suppresses cell-mediated immune reactions.
    • It binds to cyclophilin, forming a complex with calcineurin, which prevents NFATc from forming, decreasing IL-2 and T and B cell function.

    ###  Crohn's Disease and Ulcerative Colitis

    • Crohn's disease is due to an increase in T cell immunologic reaction; ulcerative colitis is due to an increase in B cell humoral reaction.
    • Glucocorticoids regulate protein, carbohydrate and fat metabolism.
    • Mineralcorticoids maintain electrolyte and volume homeostasis.
    • Acromegaly is caused by an excess of GH and IGF-I during adulthood.
    • Treatment goals for acromegaly are to decrease GH and IGF-I levels, improve signs and symptoms, and decrease the risk of complications.
    • Drug treatment options for acromegaly include GH antagonists, somatostatin (SSA) analogs, and dopamine agonists.
    • Pegvisomant is a GH antagonist that binds to GH receptors in the liver and inhibits IGF.
    • Octreotide and Lanreotide are somatostatin analogs that inhibit GH and IGF-1 production.
    • Bromocriptine is a dopamine agonist that decreases GH, IGF, and PRL levels.
    • Short stature is defined as having a height greater than 2 standard deviations below the population mean or less than the 3rd percentile for height within an age group.
    • Possible etiologies of short stature include congenital GH deficiency, acquired GH insufficiency, and idiopathic non-GH related causes.
    • Recombinant human growth factor (rhGH) is used to treat growth failure in pediatric due to inadequate GH secretion and GH deficiency in adults.
    • Cushing syndrome is caused by overproduction of cortisol.
    • Treatment options for Cushing syndrome include aminoglutethimide, metyrapone, ketoconazole, osilodrostat, mifepristone, cyproheptadine, and mitotane.
    • Addison's disease is caused by insufficient cortisol production.
    • Treatment options for Addison's disease include glucocorticoids, DHEA, and mineralcorticoids.
    • Aldosteronism is caused by excessive production of aldosterone.
    • Treatment options for aldosteronism include spironolactone, eplerenone, and amiloride.
    • Hyperprolactinemia is caused by excessive production of prolactin.
    • Treatment options for hyperprolactinemia include bromocriptine and cabergoline.
    • Glucocorticoids are used to suppress the immune system, treat inflammation, and manage certain autoimmune disorders.
    • Mineralcorticoids are used to treat hypoaldosteronism, typically due to Addison's disease.
    • Fludrocortisone is a synthetic mineralcorticoid used to treat adrenal insufficiency.
    • Glucocorticoids can cause a range of side effects, including adrenal suppression, hyperglycemia, hypertension, hypokalemia, increased risk of infection, osteoporosis, and behavioral changes.
    • Mifepristone is an antiprogesterone that can also act as a glucocorticoid receptor antagonist.
    • Cyproheptadine is a central neuromodulator that decreases ACTH release and can be used to treat Cushing syndrome in patients who have failed other therapies.
    • Renin is an enzyme produced in the kidneys that converts angiotensinogen to angiotensin I.
    • Aldosterone is a mineralcorticoid hormone that acts on the kidneys to increase sodium reabsorption and potassium excretion.
    • Amiloride is a sodium channel inhibitor used to treat aldosteronism.
    • Spironolactone and Eplerenone are aldosterone antagonists that block the action of aldosterone on the kidneys.

    Neuromuscular Blocking Agents

    • Used during surgical procedures and in intensive care units (ICUs) to produce muscle paralysis.
    • Interfere with transmission at the neuromuscular junction, preventing central nervous system (CNS) activity.
    • Used in conjunction with general anesthesia to ensure adequate ventilation, prolonged relaxation during surgical procedures, and relaxation of respiratory muscles.
    • Useful for treating status epilepticus.

    Depolarizing Neuromuscular Blocking Agent

    • Succinylcholine (Anectine®): agonist of nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction.

    Non-Depolarizing Neuromuscular Blocking Agents

    • D-Tubocurarine, Mivacurium (Mivacron®), Rocuronium (Zemuron®), Vecuronium (Norcuron®), Cisatracurium (Nimbex®): competitive antagonists of nAChR at the neuromuscular junction.
    • Cisatracurium is preferred in patients with acute respiratory syndrome (ARS) due to a lower histamine release and decreased laudanosine production, minimizing seizure episodes. It's metabolism does not depend on renal or hepatic function.

    Centrally Acting Spasmolytic Drugs

    • Baclofen (Lioresal®): GABAB agonist, inhibits motor neurons in the spinal cord.
    • Cyclobenzaprine (Flexeril®): inhibits muscle stretch reflexes in the spinal cord, causing anti-muscarinic effects.
    • Diazepam (Valium®): increases GABAergic transmission in the central nervous system, increasing interneuron inhibition of motor afferents in the spinal cord.
    • Tizanidine (Zanaflex®): α2 agonist in the spinal cord, inhibiting reflex motor output.

    Additional Spasmolytic Drugs

    • Chlorphenesin, Metacarbamol (Robaxin®), Orphenadrine (Norflex®): similar to cyclobenzaprine with varying degrees of anti-muscarinic action.

    Carisoprodol (Soma®)

    • Mechanism of Action (MOA): not fully understood, acts as a CNS depressant.
    • Clinical Use: for musculoskeletal conditions like muscle spasms, back pain, and acute pain.
    • Adverse Drug Reactions (ADRs): tolerance, dependence, withdrawal symptoms, drowsiness, tremor, agitation, headache, and depressive disorders.
    • Abuse Potential: potentially abused drug.

    Counseling Points for Spasmolytic Drugs

    • CNS Depressant Interactions: avoid use with alcohol, benzodiazepines, opioids, and other CNS depressants to prevent additive sedation, dizziness, and confusion.
    • Drug Interactions: avoid using tizanidine with ciprofloxacin and fluvoxamine due to potential increases in tizanidine levels.

    Other Spasmolytic Drugs

    • Gabapentin: anticonvulsant, used for spasticity in multiple sclerosis.
    • Pregabalin: anticonvulsant, used to relieve painful disorders.
    • Progabide: GABAA and GABAB agonist, decreases spasticity.
    • Glycine: inhibitory neurotransmitter, crosses the blood-brain barrier (BBB) and decreases spasticity.
    • Idrocilamide and Riluzole: used for treating amyotrophic lateral sclerosis (ALS), possessing spasmolytic effects by inhibiting glutaminergic transmission.

    Dantrolene (Dantrium®)

    • MOA: blocks ryanodine receptor 1 (RyR1) calcium channels in the sarcoplasmic reticulum of skeletal muscle.
    • Clinical Use:
      • Intravenous administration for malignant hyperthermia or amphetamine overdose.
      • Oral administration for spinal cord injury, cerebral palsy, and multiple sclerosis.
    • ADRs: muscle weakness, sedation.

    Neuromuscular Blocking Drugs

    • Used during surgery and in the ICU to induce muscle paralysis
    • Interfere with transmission at the neuromuscular junction, no CNS activity
    • Used with general anesthesia for adequate ventilation, prolonged relaxation during surgery, and relaxation of respiratory muscles
    • Useful for treatment of status epilepticus

    Neuromuscular Transmission

    • Influx of calcium ions (Ca2+) and release of acetylcholine (ACh)
    • ACh diffuses across the synaptic cleft and activates nicotinic acetylcholine receptors (nAChR) on the motor end plate
    • Binding of ACh to nAChR causes channel opening
    • ACh is removed from the end plate by diffusion and enzymatic degradation by acetylcholinesterase (AChE)
    • Movement of sodium (Na+) and potassium (K+) causes depolarization of the end plate membrane

    Depolarizing Neuromuscular Blocking Agents

    • Succinylcholine (Anectine®)
      • Agonist of nAChR at the neuromuscular junction
      • Initial depolarization causes transient contraction followed by prolonged flaccid paralysis
      • Hydrolyzed by plasma AChE
      • Time onset: 1-1.5 minutes
      • Duration: 5-8 minutes
      • ADRs: arrhythmias, hyperkalemia, postoperative muscle pain, increased intraocular pressure (IOP)

    Non-Depolarizing Neuromuscular Blocking Agents

    • Competitive antagonists of nAChR at the neuromuscular junction
    • Prevent depolarization by ACh, causing flaccid paralysis
    • D-tubocurarine
      • Renal elimination
      • Duration: 80-120 minutes
      • Onset: 4-6 minutes
      • ADRs: apnea, hypotension
    • Mivacurium (Mivacron®)
      • Hydrolyzed by plasma ChE
      • Duration: 12-18 minutes
      • Onset: 2-4 minutes
      • ADRs: less than D-tubocurarine, 4x potency of D-tubocurarine
    • Rocuronium (Zemuron®)
      • Hepatic metabolism
      • Duration: 20-35 minutes
      • Onset: 1-2 minutes
      • ADRs: like mivacurium, 0.8x potency of D-tubocurarine
    • Vecuronium (Norcuron®)
      • Liver metabolism, renal elimination
      • Duration: 60-90 minutes
      • Onset: 2-4 minutes
      • ADRs: like mivacurium, 6x potency of D-tubocurarine
    • Cisatracurium (Nimbex®)
      • Decreased histamine release, less laudanosine (decreased seizures), less dependence on renal and hepatic inactivation
      • Metabolism via Hofmann elimination, does not require renal or hepatic function
      • Degrades spontaneously
      • ADRs: flushing, bradycardia, hypotension
      • May improve mortality in patients with moderate or severe acute respiratory syndrome (ARS)

    Spasmolytics

    • Reduce spasticity in various painful conditions
    • Also called “centrally acting” muscle relaxants
    • Treat chronic pain, painful fibromyalgia, or acute spasm due to muscle injury or inflammation in stroke, multiple sclerosis, and cerebral palsy patients

    Centrally Acting Spasmolytics

    • Baclofen (Lioresal®)
      • GABAB agonist, spinal inhibition of motor neurons
      • Pre and post synaptic inhibition of reflex motor output
      • Oral, intrathecal
      • ADRs: sedation, weakness
    • Cyclobenzaprine (Flexeril®)
      • Inhibits muscle stretch reflex in the spinal cord
      • Decreased hyperactive muscle reflexes
      • Anti-muscarinic effect
      • Hepatic metabolism
      • Duration: 4-6 hours
      • ADRs: anti-muscarinic effects, sedation
    • Diazepam (Valium®)
      • Increased GABAergic transmission in the CNS
      • Increased interneuron inhibition of motor afferents in the spinal cord
      • GABAA agonist
      • Hepatic metabolism
      • Duration: 12-24 hours
      • ADRs: depressant effects, dependence, sedation
    • Tizanidine (Zanaflex®)
      • ɑ2 agonist in spinal cord
      • Pre and post synaptic inhibition of reflex motor output
      • Renal and hepatic elimination
      • Duration: 3-6 hours
      • ADRs: weakness, sedation, hypotension

    Other Spasmolytics

    • Chlorphenesin, metacarbamol (Robaxin®), orphenadrine (Norflex®)
      • Similar to cyclobenzaprine with varying degrees of anti-muscarinic action

    Carisoprodol (Soma®)

    • MOA: not clear, acts as a CNS depressant
    • Used for musculoskeletal muscle spasms, back pain, and acute pain relief
    • Standard dose: 350 mg 3-4 times per day
    • Potential abuse like other class IV drugs
    • ADRs: tolerance, dependence, withdrawal symptoms, drowsiness, tremor, agitation, headache, depressive disorder
    • One of the most diverted and abused drugs
    • Controlled substance (CS) IV as of January 2012
    • Metabolized to meprobamate (substance with barbiturate-like properties)
    • Pregnancy category C
    • DDIs: ethanol increases depressant effects, CYP2C19

    Counseling Points for Spasmolytics

    • Be cautious when using with CNS depressants like alcohol, benzodiazepines, and opioids
    • Avoid alcohol, sleeping pills, antihistamines, sedatives, pain pills, and tranquilizers except under doctor supervision
    • Avoid using tizanidine with ciprofloxacin or fluvoxamine (can increase tizanidine levels)

    Additional Spasmolytics

    • Gabapentin: anticonvulsant, useful as spasmolytic in MS
    • Pregabalin: anticonvulsant, relieves painful disorders
    • Progabide: acts as a GABA A and GABA B agonist, decreases spasticity
    • Glycine: inhibitory neurotransmitter that can cross the blood-brain barrier (BBB), decreases spasticity
    • Idrocilamide and Riluzole: for treatment of ALS, have spasmolytic effects. Work by inhibiting glutaminergic transmission

    Dantrolene (Dantrium®)

    • MOA: blocks ryanodine receptor 1 (RyR1) calcium channel in the sarcoplasmic reticulum of skeletal muscle
    • Effect: decreased actin-myosin interaction, weakens skeletal muscle contraction
    • Used IV for malignant hyperthermia or overdose of amphetamines
    • Rarely a heritable disorder triggered by general anesthetics and succinylcholine
    • Sudden and prolonged release of calcium, causing massive muscle contraction, increased lactic acid, and increased body temperature
    • Treatment for malignant hyperthermia: control body temperature, lactic acidosis, and use dantrolene to reduce calcium release
    • Used orally for spinal cord injury, cerebral palsy, and multiple sclerosis
    • ADRs: muscle weakness, sedation

    Summary of Study Notes

    • People undergoing surgery may be given depolarizing agents like succinylcholine and non-depolarizing agents like D-tubocurarine, rocuronium, or vecuronium.
    • Cerebral palsy may be treated with spasmolytics like baclofen, cyclobenzaprine, diazepam, or tizanidine.
    • Dantrolene works by blocking calcium channels and is useful for malignant hyperthermia due to amphetamine overdose or during anesthetic administration. It is a muscle relaxant.
    • Cisatracurium is a non-depolarizing neuromuscular blocker that has advantages such as decreased histamine release, less laudanosine (which decreases seizures), and less hepatic elimination.

    Hyperfunctional & Hypofunctional Glands

    • Hyperfunctional glands include Hyper-PRL (pituitary), Acromegaly (pituitary), Cushing syndrome (adrenal), and Hyperaldosteronism (adrenal).
    • Hypofunctional glands include Hypogonadism (pituitary), Hypo-PRL (pituitary), Short stature (pituitary), Addison’s (adrenal), 2nd adrenal insufficiency (adrenal), and Hypoaldosteronism (adrenal).

    Hormone Actions

    • Hypothalamic hormones stimulate or inhibit the anterior pituitary to release hormones that target specific organs.
    • Most hormones act through G protein coupled receptors in the pituitary, except GH and prolactin, which act through JAK/STAT receptors.
    • Target organ hormones often act through a superfamily of nuclear receptors.

    Hormone Types

    • Amine hormones are derived from tyrosine or tryptophan, examples include Norepinephrine, Epinephrine, T4, T3, melatonin, dopamine.
    • Polypeptide/protein hormones are chains of amino acids, examples include ADH, GH, insulin, oxytocin, glucagons, ACTH, PTH, LHRH.
    • Glycoproteins hormones have peptide and oligosaccharide chains, examples include LH, FSH, TSH, EPO.
    • Steroids are lipids derived from cholesterol, examples include Testosterone, estrogen, progesterone, glucocorticoids, mineralcorticoids, 1,25 dihydrocalciferol (vit D).

    Acromegaly

    • Acromegaly is caused by increased production of GH and IGF-I during adulthood.
    • Treatment goals include decreasing GH and IGF, improving signs and symptoms, and minimizing the risk of complications associated with mortality.
    • Drugs used to treat acromegaly include GH antagonists, somatostatin (SSA) analogs, and dopamine agonists.
    • Possible etiologies of acromegaly include a GH-secreting pituitary adenoma, ectopic GH-secreting adenoma, and excess GHRH secretion.

    GH Antagonist

    • Pegvisomant (Somavert®) binds to GH receptors in the liver and inhibits IGF.
    • Does not inhibit GH production but blocks the physiologic effects of GH on target tissues.
    • ADRs include hepatoxicity, LFT, nausea, diarrhea, and pain at the injection site.
    • Dose adjustment is necessary in hepatic impairment.

    Somatostatin Analogues (SSA)

    • Inhibit GH and IGF1.
    • 45 times more potent than endogenous somatostatin.
    • Also inhibit gastrin, insulin, and glucagon, which could cause hypoglycemia or hyperglycemia.
    • Drugs include Octreotide and Lanreotide.
    • ADRs include nausea, flatulence, gallstones, bradycardia, vitamin B12 deficiency, chest pain, hyperglycemia in type II DM, severe hypoglycemia in type I DM, malaise, fever, and diarrhea/abdominal discomfort.

    Dopamine

    • Decreases GH, IGF, and PRL.
    • Bromocriptine (Parlodel®) duration is shorter for acromegaly treatment; longer for hyperprolactinemia.
    • Can suppress local immune response against H pylori, leading to its reactivation.

    Glucocorticoid ADRs

    • Weight gain: Stimulates lipolysis, leading to increased fatty acids and fat deposition.
    • Increased serum glucose by inhibiting reuptake of glucose by muscle and increasing appetite.
    • Glaucoma, cataracts: Increased intraocular pressure.
    • Iatrogenic Cushing syndrome: Fat distribution in the back, neck, and face (moon face). Serious metabolic changes can occur, such as myopathy, diversion of amino acids to glucose production, hyperglycemia, osteoporosis, and others.
    • Retard growth: Decreases osteoblast precursors during skeletal growth, suppressing growth. Natural glucocorticoids have less growth-suppressing potency than synthetic ones, even at equivalent doses.

    Cushing Syndrome & Mitigation

    • Drug-induced Cushing syndrome can be caused by glucocorticoids (primarily oral therapy), medroxyprogesterone acetate, and OTC/herbals (e.g., topical hydrocortisone, magnolia bark, adrenal cortex extracts).
    • To avoid Cushing syndrome, administer the lowest possible dose, continue therapy for the shortest duration, utilize routes with minimal systemic absorption, administer every other day in the morning, avoid medications that inhibit glucocorticoid metabolism, and gradually decrease the dose.
    • Full recovery of the HPA axis may take up to one year after discontinuing corticosteroids; supplementation may be necessary during periods of acute stress.

    Hyperprolactinemia

    • Hyperprolactinemia can be caused by antipsychotics, DA antagonists, metoclopramide, TCAs, MAOIs, SSRIs, H2 blockers, verapamil, and methyldopa.
    • Symptoms in females include acne, amenorrhea, decreased libido, hirsutism, infertility, galactorrhea, and osteoporosis.
    • Symptoms in males include decreased libido, erectile dysfunction, galactorrhea, gynecomastia, infertility, and loss of muscle mass.

    Dopamine Agonist Comparison

    • Bromocriptine is less costly but less effective in decreasing PRL levels and tumor size. It is preferred for patients desiring pregnancy but requires multiple doses daily and can cause headaches, dizziness, GI discomfort, and postural hypotension.
    • Cabergoline is more effective in decreasing PRL and tumor size, restoring gonadal function, has increased tolerability, and is administered 1-2 times per week. However, it is more costly, and its efficacy is not established beyond 2 years.

    Assessment and Management

    • Minimum 1 year of therapy for hyperprolactinemia is recommended.
    • Monitor serum PRL every 6-12 months once symptoms resolve.
    • If normal PRL levels are maintained for ≥ 2 years with decreased tumor size, consider withdrawing the agent to determine if the patient has achieved remission.

    Summary Answers

    1. Drugs that cause increased PRL include antipsychotics, DA antagonists, metoclopramide, TCAs, MAOIs, SSRIs.
    2. Spironolactone is useful to treat Aldosteronism, hyperkalemia, hypokalemia, and edema.
    3. Symptoms of Addison's disease include fatigue, weakness, hypotension, anorexia, weight loss, and hyperpigmentation.
    4. Derivatives of cholesterol compounds include testosterone, estrogen, progesterone.

    Glucocorticoid ADRs and Supplementation

    1. ADRs of corticosteroids include weight gain, hyperglycemia, osteoporosis, muscle weakness, electrolyte imbalances, and iatrogenic Cushing syndrome.
    2. Supplementation with calcium, vitamin D, potassium, bisphosphonates, and probiotics are important when taking corticosteroids.
    • Growth hormone related agents include pegvisomant, octreotide, lanreotide, and bromocriptine.

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    This quiz covers essential information about psychostimulants used for treating ADHD, including their effects on core symptoms and specific medications like Adderall XR and Desoxyn. Learn how these substances operate in the brain and their impact on behavior and academic performance. Additionally, the course will touch upon the distinction between psychostimulants and psychomimetics.

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