Drug Classes and Mechanisms of Action
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Questions and Answers

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

Cortisone binds to CGR in the cytoplasm, dimerises, and then translocates to the nucleus.

What are two adverse effects associated with corticosteroids like hydrocortisone?

Immunosuppression and hyperglycemia.

Describe the significance of tapering off corticosteroids.

Tapering is necessary to avoid withdrawal symptoms and allow the adrenal glands to resume normal function.

What class of drugs does carbimazole belong to, and what is its MOA?

<p>Carbimazole is a thyrostatic agent that competes with oxidised iodide in the colloid space.</p> Signup and view all the answers

How does propylthiouracil (PTU) differ from carbimazole in terms of its action?

<p>PTU also inhibits the conversion of T4 to T3 in addition to affecting iodide in the colloid.</p> Signup and view all the answers

What adverse effect is specifically associated with the use of corticosteroids like prednisolone?

<p>Peptic ulcers.</p> Signup and view all the answers

What role do mineralocorticoids like fludrocortisone play?

<p>Fludrocortisone binds to GRE to alter transcription and regulate sodium and water retention.</p> Signup and view all the answers

Identify one important consideration in the administration of corticosteroids.

<p>Patients should be monitored for signs of immunosuppression.</p> Signup and view all the answers

What is the mechanism of action of sulfonylureas like Glimepiride?

<p>Sulfonylureas inhibit the SUR-1 subunit of the K/ATP channel, causing membrane depolarization and increasing insulin secretion.</p> Signup and view all the answers

What are common side effects associated with the use of sulfonylureas?

<p>Common side effects include hypoglycemia and weight gain.</p> Signup and view all the answers

Describe the role of SGLT2 inhibitors such as Dapagliflozin in glucose management.

<p>SGLT2 inhibitors block the reabsorption of glucose in the kidneys, leading to increased excretion of glucose in urine.</p> Signup and view all the answers

Identify two potential adverse effects of SGLT2 inhibitors.

<p>Potential adverse effects include urinary tract infections (UTIs) and dehydration.</p> Signup and view all the answers

What is the overall outcome of inhibiting the SGLT2 transporter?

<p>Inhibiting the SGLT2 transporter leads to decreased reabsorption of glucose and promotes weight loss.</p> Signup and view all the answers

How do sulfonylureas affect insulin secretion?

<p>Sulfonylureas increase insulin secretion from the pancreas by closing the K/ATP channels.</p> Signup and view all the answers

Explain why weight gain is a concern for patients taking sulfonylureas.

<p>Weight gain is a concern because it may counteract the benefits of glucose control and worsen overall health.</p> Signup and view all the answers

What mechanism does Orlistat use to affect fat digestion?

<p>Orlistat binds to pancreatic lipase, preventing the hydrolysis of fat.</p> Signup and view all the answers

What are some side effects associated with the use of Orlistat?

<p>Common side effects include cramping, flatulence, and fecal incontinence.</p> Signup and view all the answers

In what way can SGLT2 inhibitors aid in weight loss?

<p>By promoting the excretion of glucose in urine, SGLT2 inhibitors help reduce caloric intake and promote weight loss.</p> Signup and view all the answers

How do sympathomimetics like Phentermine affect appetite?

<p>Phentermine suppresses appetite by indirectly stimulating noradrenergic pathways in the central nervous system.</p> Signup and view all the answers

What potential cardiovascular effects may be caused by the use of sympathomimetics?

<p>They can lead to increased blood pressure and overstimulation of the cardiovascular system.</p> Signup and view all the answers

What type of drug is alginate and what is its role?

<p>Alginate is a component of antacids that helps manage symptoms of acid reflux.</p> Signup and view all the answers

What is the risk of taking antacids along with other medications?

<p>Antacids can change the absorption of other drugs, affecting their efficacy.</p> Signup and view all the answers

What is the main action of Orlistat in regards to fat absorption?

<p>Orlistat prevents the absorption of fat by inhibiting the enzyme responsible for breaking down fats.</p> Signup and view all the answers

What should individuals using Orlistat be cautious about regarding vitamins?

<p>They should be careful with vitamin deficiency due to reduced absorption of fat-soluble vitamins.</p> Signup and view all the answers

What is the primary function of Estradiol in menopause hormone therapy?

<p>It replaces estrogen in the body.</p> Signup and view all the answers

What risks are associated with long-term use of Estradiol?

<p>It increases the risk of breast cancer and endometrial cancer.</p> Signup and view all the answers

What type of drug is Bazedoxifene and what are its effects on endometrial cancer risk?

<p>Bazedoxifene is a SERM that reduces the risk of endometrial cancer.</p> Signup and view all the answers

How does Bazedoxifene interact with breast tissue?

<p>It acts as an estrogen antagonist.</p> Signup and view all the answers

What is the nature of Tibolone as a hormone therapy option?

<p>Tibolone is a STEAR, whose metabolites act as estrogen on bone.</p> Signup and view all the answers

What side effects are associated with the use of Tibolone?

<p>Increased risk of acne and facial hair.</p> Signup and view all the answers

How does the use of progesterone affect the risks associated with Estradiol?

<p>Progesterone decreases the risk of endometrial cancer.</p> Signup and view all the answers

In what ways does Estradiol impact metabolism in the body?

<p>It increases metabolism via CYP3A4.</p> Signup and view all the answers

How do anticholinergics function regarding acetylcholine?

<p>Anticholinergics block acetylcholine from binding to muscarinic receptors.</p> Signup and view all the answers

What is the primary effect of botulinum toxin A on neuromuscular transmission?

<p>Botulinum toxin A blocks the release of acetylcholine.</p> Signup and view all the answers

Describe the mechanism by which dantrolene decreases muscle contraction.

<p>Dantrolene decreases muscle contraction by preventing calcium release, which inhibits binding to troponin.</p> Signup and view all the answers

What neurotransmitters are affected by amphetamines?

<p>Amphetamines inhibit the transporters for dopamine, norepinephrine, and serotonin.</p> Signup and view all the answers

What effects can lisdexamfetamine have on heart rate and blood pressure?

<p>Lisdexamfetamine can increase heart rate and blood pressure.</p> Signup and view all the answers

How do amphetamines affect appetite?

<p>Amphetamines have anorectic effects, suppressing appetite.</p> Signup and view all the answers

What distinguishes dexamphetamine from other amphetamines?

<p>Dexamphetamine has a shorter duration of action compared to some other amphetamines.</p> Signup and view all the answers

Explain the role of acetylcholine in muscle contraction.

<p>Acetylcholine binds to receptors on muscle fibers, triggering a cascade that leads to contraction.</p> Signup and view all the answers

What is the role of sphingosine 1-phosphate receptor modulators in the immune system?

<p>They prevent lymphocytes from leaving lymph nodes, decreasing their infiltration into the CNS.</p> Signup and view all the answers

How does Fingolimod affect the movement of lymphocytes?

<p>Fingolimod prevents lymphocytes from exiting lymph nodes, which reduces their presence in the CNS.</p> Signup and view all the answers

What condition do the side effects rash and alopecia relate to among the discussed therapies?

<p>These side effects relate to the use of Teriflunomide.</p> Signup and view all the answers

What mechanism does Teriflunomide employ to reduce activated T and B cells in the CNS?

<p>It inhibits DHODH, decreasing the number of activated T and B cells.</p> Signup and view all the answers

Which dopaminergic agent is known to cross the Blood-Brain Barrier (BBB) and act as dopamine?

<p>Levodopa crosses the BBB and is converted to dopamine in the brain.</p> Signup and view all the answers

What impact does the mechanism of sphingosine 1-phosphate receptor modulators have on bradycardia?

<p>These modulators can cause bradycardia as a side effect due to their effects on heart rate.</p> Signup and view all the answers

Identify one outcome of inhibiting lymphocyte migration with receptor modulators.

<p>It decreases the infiltration of lymphocytes into the central nervous system (CNS).</p> Signup and view all the answers

What is a significant therapeutic goal when using drugs like Ozanimod in the context of autoimmune diseases?

<p>The goal is to prevent lymphocyte migration to reduce CNS inflammation.</p> Signup and view all the answers

Study Notes

Drug Classes and Mechanisms of Action

  • Corticosteroids: Bind to glucocorticoid receptors (GRs) in the cytoplasm, dimerize, translocate to the nucleus, and bind to GREs to alter gene transcription. Effect includes immunosuppression, peptic ulcers, hyperglycemia, and hepatic damage. Tapering is necessary.

  • Thyroid Hormone Synthesis Inhibitors: Compete with iodine, inhibiting its oxidation and reaction with thyroglobulin, therefore blocking thyroid hormone synthesis. Propylthiouracil also inhibits the conversion of T4 to T3. Carbimazole has a longer half-life.

  • Thyroid Hormone Release Inhibitors: Concentrated iodine transiently inhibits TH release, restoring negative feedback loops.

  • Thyroid Hormones: Restore negative feedback loops. High iodine levels may increase, while over treating might cause increased blood pressure, heart rate, arrhythmia and decreased bone mineral density..

  • Vitamins (Calcium): Essential for bone formation and density. Increases calcium absorption, mobilizes calcium. Should be taken at night. A risk of hypercalcemia exists. Avoid with calcium or iron supplements to prevent absorption interference

  • Bisphosphonates: Prevent osteoclasts from binding to bone, reducing bone loss and osteoblast apoptosis. Avoid with other drugs like calcium and iron supplements and digoxin, levothyroxine to lessen the risk of interference.

  • HRT (Hormone Replacement Therapy): Oestrogen agonists increase bone mineral density, act like estrogen.

  • RANK Ligand Inhibitors: Bind to RANKL, preventing the binding of RANKL to its receptor and thus reducing osteoclast synthesis and formation, reducing bone resorption.

  • Recombinant PTH: Increases calcium absorption. Decreases its elimination. Increases osteoblast formation and inhibits apoptosis.

  • Anti-sclerostin: Inhibits sclerostin, which inhibits bone formation and activates bone resorption.

  • Antiepileptics: Inactivate vitamin D, decreasing calcium absorption.

Endocrine Effects and Other Considerations

  • Diabetes Medications: Various classes of drugs work in different ways affecting blood glucose control, but some will increase insulin sensitivity, increase glucose uptake in cells, inhibit glucose reabsorption, or mimic endogenous GLP-1 effects. Some have adverse effects like nausea, vomiting or dehydration; patients with renal impairment need dosage adjustments.

  • Gastrointestinal Effects: Various medications have adverse effects including diarrhea, constipation, nausea, vomiting, flatulence. Some have to be taken at night.

  • Other Considerations: Some drugs, (e.g., with calcium), should be taken at a specific time, and should avoid other drugs due to possible interaction risk. Others have long half-lives, or poor oral bioavailability. Patients should work with their doctor to understand potential interactions. Drug interactions can affect the absorption of other drugs.

Additional Drug-Specific information (from pages 2-6)

(Note this section includes a broad range of drugs and conditions, the study notes do not attempt to give a thorough overview of all mentioned medications but highlight key factors)

  • Anti-muscarinic Agents: Work by inhibiting muscarinic receptors, have side effects like constipation, dry mouth, and blurred vision. Some may also cross the blood-brain barrier

  • Anti-spasmodic agents: Reduce inflammation and muscle spasms and their effects.

  • Antidepressants: Many classes (SSRI, SNRI, TCAs), inhibit reuptake of serotonin, noradrenaline, or other neurotransmitters, which leads to increased levels of these neurotransmitters in the synapse. Potential side effects vary.

  • Anti-inflammatory Agents: Such as 5-aminosalicylates, used in intestinal inflammation.

  • Contraceptives: Suppression of GnRH, FSH and LH prevents the production of sex hormones, which prevents ovulation.

  • Emergency Contraceptives: Various mechanisms prevent or delay ovulation.

  • Anti-psychotics: Affect multiple neurotransmitters.

  • Other Medications: Page 6 contains many other unique drugs with some having specific mechanisms of actions and side effects. Various therapeutic and pathological information is present throughout the document and should be approached by individual drug focus for a more comprehensive understanding.

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Description

Explore the various drug classes and their mechanisms of action, including corticosteroids, thyroid hormone synthesis inhibitors, and vitamins essential for bone health. This quiz covers how these substances impact human physiology and the necessary monitoring involved in their use. Test your knowledge on pharmacology and drug interactions.

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