Pharmacology Exam 3 Study Guide PDF

**FDA warning on all antidepressants** ALL categories of antidepressants\ ♣ Increased risk of suicidal thoughts and behavior\ ♣ Children, adolescents, young adults up to 24 years of age\ ♣ First two months of treatment\ ♣ Depression and psychiatric illness risk factors 2. **SSRI medications**...

**FDA warning on all antidepressants** ALL categories of antidepressants\ ♣ Increased risk of suicidal thoughts and behavior\ ♣ Children, adolescents, young adults up to 24 years of age\ ♣ First two months of treatment\ ♣ Depression and psychiatric illness risk factors 2. **SSRI medications** a. Citalopram b. Escitalopram c. Fluoxetine -- First in USA to be approved for depression, inhibitors of CYPP450 d. Fluvoxamine -- only OCD in USA e. Paroxetine - inhibitors of CYPP450 f. Sertraline No specific monitoring with the exception of closely monitor for the first 2-3 weeks after initiation for assessment of suicidal ideation. 3. **What herbs interact with SSRI** Ginkgo Biloba [St. John\'s Wort] Garcinia cambogia (HCA) L-tryptophan (or 5-HTP) [SAMe (S-adenosyl-methionine) supplements.] Increase the risk for serotonin syndrome 4. **Onset of action of SSRI** Onset of action two weeks, up to 12 weeks for maximum benefit. T ½ 16-36 hours 5. **Mechanism of action of SSRI** 6. **Indications for SSRI** All SSRIs but fluvoxamine g. Depression h. Anxiety i. Panic disorders j. OCD k. Bulimia, off label anorexia l. Premenstrual dysphoric disorder m. PTSD n. Generalized anxiety social phobia 7. **Which medications are SNRI's** - - - - - - Mechanism of Action: Inhibit the reuptake of Serotonin &Norepinephrine - contraindicated in patients who received monoamine oxidase inhibitors (MAOIs) in the previous two weeks because of drug-drug interactions that cause the serotonin syndrome 8. **MOA of Desvenlafaxine a SNRI** o. Block reuptake of serotonin and norepinephrine p. Degree of the block is based upon dosage Glucuronidation excretion Hepatic and Renal Dose adjustment hepatic and renal impairment 9. **Side effects of SNRI** q. Common i. CNS ii. Nausea, constipation iii. Dry mouth iv. Sexual r. Higher dosages v. hypertension s. Similar to Venlafaxine t. Palpitation ADE Levomilnacipran u. Similar to others v. Urinary hesitation due to the dual mechanism of action SNRI and TCA may be effective in relieving pain such as HA or backpain associated with depression. They may also be affective in the treatment of diabetic neuropathy, postherpetic neuralgia, fibormyalgia, and low back pain. 10. **Side effects of mirtazapine** Atypical antidepressants - Mirtazapine enhances serotonin and norepinephrine neurotransmission - Sedation, increased appetite and weight gain 11. **Which medications are tricyclic antidepressants** w. Imipramine Trimipramine Nortriptyline Doxepin x. Desipramine Amitriptyline Clomipramine Protriptyline Amoxapine 12. **Indications for tricyclic antidepressants** Depression, panic disorder, prevent migraine, treat chronic pain syndrome 13. **Dosing of tricyclic antidepressants when used for neuropathic pain** *[Amitriptyline]* and duloxetine. Lower the dose. Commonly, amitriptyline is initiated at low doses, typically between 5-10 mg/day, to assess tolerance and efficacy. Amitriptyline\'s analgesic effects are attributed to its ability to inhibit norepinephrine reuptake, which activates α1- and α2-adrenergic receptors, crucial for pain modulation 14. **Which anxiolytic to choose based on sleep patterns** For patients with sleep onset insomnia, a relatively short-acting medication is a reasonable choice for an initial trial of pharmacologic therapy.. zaleplon, zolpidem, triazolam, and ramelteon, temazepam, Eszopiclone. For patients with sleep maintenance insomnia, a longer-acting medication is preferable for an initial trial of pharmacologic therapy. zolpidem extended release, eszopiclone, temazepam, lorazepam, eszopiclone, low dose doxepin, and suvorexant. Longer-acting medications may increase the risk for hangover sedation. For patients with awakening in the middle of the night, both zaleplon and a specific sublingual tablet form of zolpidem have been developed for use during the night, with the constraint that there will be at least four hours of time in bed remaining after administration. 15. **Side effects of medications use to help patients sleep** Drowsiness and confusion, ataxia, cognitive impairment, sleepwalking/driving, anterograde amnesia, dizziness, HA, dry mouth peripheral edema somnolence, suicidal ideation 16. How to dose anxiolytics in the elderly and patients with sleep impairment (eszopiclone) Elderly and hepatic impairment decrease dose, Max 2mg 17. **Mechanism of action of zolpidem** y. Binds to GABAa Receptors z. Relative selectivity for α₁ subunit Has fewer withdrawal symptoms, minimal rebound insomnia and minor tolerance 18. **ADE associated with melatonin receptor agonists** vi. HA vii. Increased LFT viii. Abnormal dreams Include ramelteon and tasimelteon, agonist for MT1&2 19. **Goals and outcomes of treatment of anti-Parkinson's medications** Goal: restoring dopamine in the basal ganglia and antagonizing the excitatory effect of cholinergic neurons, end with correct dopamine/acetylcholine balance No drugs stop the progression or reverse the disease Management of individual patients requires careful consideration of a number of factors, including the patient\'s symptoms and signs, age, stage of disease, degree of functional disability, and level of physical activity and productivity 20. **Role of carbidopa and levodopa** Levodopa actively transported into the CNS where it is converted into dopamine Carbidopa Inhibits the metabolism of levodopa outside of the CNS 21. **Which medications are Monoamine oxidase type B inhibitors** Selegiline- administered with levodopa to enhance its effects. Metabolized to methamphetamine\ Rasagiline- 5x more potent than selegilin\ Safinamide -- used with levodopa/carbodopa 22. **Side effects associated with tolcapone** Tolcapone Prevents competition for transport of levodopa by 3-O-methyldopa. With a long duration of action. When with levo/carbo side effects include:\ Diarrhea, orthostatic hypotension\ Nausea, anorexia, dyskinesias, hallucinations, sleep disorders\ Tolcapone-hepatic necrosis 23. **Goal of treatment with donepezil in patients with Alzheimer's disease** Donepezil is an acetylcholinesterase inhibitor. That improves cholinergiv transmission and can cause cramps NVD tremors Goals of therapy Improve cholinergic transmission with the CNS Prevent excitotoxic actions from overstimulation of NMDA-glutamate receptors Reality Palliative Short-term none alter the disease process 24. **Side effects associated with memantine** Memantine blocks NMDA receptors prevents toxic CA levels. Side effects: Confusion, agitation, restlessness (similar to symptoms of Alzheimer's\ Disease) 25. **Common causes of neuropathic pain** Results from damage to or pathology with the nervous system Central or peripheral Causes diabetes mellitus Post-herpetic neuralgia Stroke Alcoholic neuropathy Cancer-related pain/treatment Phantom limb pain Trigeminal neuralgia Vitamin B₁₂ deficiency 26. **ADE's associated with gabapentin** Gabapentin/pregabalin is an anticonvulsant that is also used for neuropathic pain. It binds to CA channels. Preg is better absorbed. Side effects include: dizziness, drowsiness, fatigue, peripheral edema 27. **Duration of a trial of gabapentin to treat neuropathic pain** For chronic use a trial may be required that lasts 2 months or more. PREg is faster onset. 28. **Specific therapy for managing trigeminal neuralgia** Carbamazepine is a first like therapy for trigeminal neuralgia. It prevents repeated discharge in neurons to relieve pain. Related to TCAs TCAs have anticholinergic and antihistaminergic effects. Like SNRIs, there effects on serotonin and norepinephrine reuptake inhibitors are what helps. TCAs needed a lower dose that what is used for depression and the effects can last for 1-3 weeks. The SNRIS specifically Venlafaxine: acute and chronic neuropathic pain. And Duloxetine: painful diabetic neuropathy, fibromyalgia, and more recently chronic low back pain and osteoarthritis. Do not forget about the ADE of dry mouth insomnia drowsiness and constipation 29. **Mechanism of action of capsaicin cream** The repeated application will deplete substance p from the primary afferent neurons. Watch for any burning or stinging or erythema. The patch works fast in an hour. The cream can take 6-8 weeks while being applied 3-4 times a day/ 30. **Ketamine dosing with a patient on chronic opioids** Ketamine reduces firing of NMDA receptors. its dosing is lower than anesthesia dose. When using for anesthesia you can not use it one infants less than 3month or known/suspected schizophrenia. May need to use doses at the higher range in opioid-tolerant patients. Reduce baseline opioids by 25% to 50% when used concomitantly with ketamine. Watch for agitation. Confusion. Hallucinations, vivid imagery. 31. **Topical lidocaine** Lidocaine is used as adjunctive or sometimes alone. It is for localized neuropathic pain. It will block initiation and conduction of nerve impulses and this is done by decreasing permeability to NA ions and inhibiting depolarization. It usually happens over about 4 hours. 32. **Mechanism of action of gabapentin in the management of epilepsy** Narrow spectrum for focal epilepsy Enhance Inhibition of gabaergic impulses Non- inducer oral contraceptive Attaches to the a2Bsubunit 33. **Side effects of levetiracetam** CNS Depression- almost all Suicidal Ideation Blood dyscrasias Steven Johnson Syndrome Nausea Weight gain/loss Hepatic failure 34. **Contraindications to phenytoin** Pregnancy, liver problems. Sinus bradycardia, drug interactions, hypersensitivity 35. **Monitoring parameters of carbamazepine history of bone marrow depression** Carbamazepine can lead to leukopenia, thrombocytopenia, and agranulocytosis. We need to do regular blood count assessments. Look for WBC below 3000 or neutrophil count below 1500 36. **Drug interactions of valproic acid with other antiepileptics** 37. **What are key concerns when prescribing antiepileptics to pregnant women** sodium valproate and phenytoin, are associated with an increased risk of major congenital malformations Women taking AEDs are often advised to take higher doses of folic acid (5mg daily) before conception and during the first trimester to reduce the risk of neural tube defects 38. **Mechanism of action of lamotrigine** Broad spectrum sodium channel inhibitor. That prevents repetitive firing of neurons that lead to seizures. enhances GABAergic neurotransmission while inhibiting glutamate release, further contributing to its anticonvulsant properties 39. **Common side effects of topiramate** 40. **Contraindications to valproic acid** Liver Disease: Valproic acid should not be used if you have liver disease or significant hepatic dysfunction. Urea Cycle Disorders: It is contraindicated in individuals with urea cycle disorders. Genetic Mitochondrial Disorders: This includes conditions like Alpers\' disease or Alpers-Huttenlocher syndrome, especially in children younger than 2 years old. Allergy: If you are allergic to valproic acid or any of its components. Pregnancy: It should be avoided during pregnancy unless absolutely necessary, as it can cause birth defects and decreased IQ in the baby. 41. **Monitoring parameters of ethosuximide with concomitant psychologic diseases** Therapeutic drug monitoring helps in adjusting ethosuximide doses based on individual plasma concentrations, which can vary significantly among patients. Ethosuximide has been associated with psychological disturbances, particularly in children and adolescents, where it may lead to profound intellectual and affective issues. For women of childbearing age, monitor pregnancy status regularly, as ethosuximide can have implications for pregnancy 42. **Which antiepileptic interferes with oral contraceptives** carbamazepine, phenytoin, and topiramate. These drugs primarily act as inducers of the hepatic cytochrome P450 enzyme system, which can significantly reduce the plasma levels of contraceptive hormones. 43. **Which antiepileptics are safest during pregnancy** safest during pregnancy are **lamotrigine** and **levetiracetam**. Studies have shown that these medications are associated with a lower risk of major congenital malformations compared to other antiepileptics 44. **Common side effects associated with phenytoin** Drowsiness and confusion Slurred speech Abnormal eye movements Problems with balance, coordination, or muscle movement Nausea and vomiting Dizziness Tremors or shaking Gingival hyperplasia (overgrowth of the gums) Skin rashes 45. **Primary mechanism of action of COX-1 inhibitors leading to GI bleeding** COX-1 is expressed in most tissues but variably. It is described as a \"housekeeping\" enzyme, regulating normal cellular processes (such as gastric cytoprotection, vascular homeostasis, platelet aggregation, and kidney function), and is stimulated by hormones or growth factors. Gastric cytoprotection is what combats ulcers by increasing mucosal protection. 46. **Primary indications for COX-2 inhibitors** COX-2 is a highly regulated enzyme that is constitutively expressed in the brain, kidney, and bone, but which is undetectable in most other tissues increased during states of inflammation inhibited by glucocorticoids 47. **What is nociceptive pain?** Nociceptive pain is often due to musculoskeletal conditions, inflammation, or mechanical/compressive problems. In contrast to neuropathic pain, the pharmacologic approach to nociceptive pain primarily involves nonnarcotic and opioid analgesia. Medication is used in conjunction with non-pharmacologic therapies and approaches to relieve the source of the pain 48. **Opioids are useful in the treatment of which type of pain** moderate to severe pain. This includes pain resulting from: Post-surgical pain: Pain following surgical procedures. Cancer-related pain: Pain associated with cancer or its treatment. Severe trauma or injury: Pain from serious injuries, such as fractures or burns. Chronic pain conditions: Pain that persists over a long period and hasn\'t responded well to other treatments. Breakthrough pain: Sudden, intense spikes of pain that occur despite ongoing pain management. 49. **MOA of NSAIDS** Indicated for mild to moderate pain, strain, and sprain. When combined with opioids the produce a dose-sparing effect. NSAIDs inhibit cyclooxygenase so there is no transformation of arachidonic caid to prostaglandins which leads to an anti-inflammatory response. Included are aspirin, celecoxib/cox-2l, diclofenac, ibuprofen, PGE₂ sensitizes nerve endings to the action of bradykinin, histamine, and other chemicals that are locally released during the inflammation process, NSAIDs inhibit the production of PGE₂, Antipyretic PGE₂ can elevate the set point of the anterior hypothalamic thermoregulatory center. Inhibition of prostaglandin formation helps restore normal regulation ketorolac,meloxicam,naproxen,piroxicam. 50. **Mechanism of action of naloxone** Naloxone is an opioid antagonist the reverses the effects of opioid overdose. Its mechanism of action involves competitive displacement of opioid agonists at the μ-opioid receptor (MOR), effectively restoring normal respiratory function without fully reversing consciousness. 51. **Opioids MOA for pain** Opioids bind to mu, delta, and kappa receptors, predominantly mu receptors, which are responsible for analgesia. This binding activates intracellular signaling pathways, inhibiting the release of neurotransmitters involved in pain transmission, thus reducing the perception of pain. They stimulate the release of the body\'s own natural pain-relieving compounds, known as endogenous opioids (like endorphins). 52. **Risk discussion with patients being prescribed opioids**  Long-term use raises concerns about tolerance, dependence, and serious side effects, including respiratory depression and overdose. 53. **Benefits of medicated patches** Targeted Relief: They deliver medication directly to the area of pain, providing localized relief without affecting the entire body. Controlled Release: The medication is released slowly over time, maintaining a consistent level of pain relief. Convenience: Patches are easy to use and can be worn for several days, reducing the need for frequent dosing. Reduced Side Effects: By targeting specific areas, patches can minimize systemic side effects compared to oral medications. Non-Invasive: They provide an alternative to injections or oral medications, which can be beneficial for patients who have difficulty swallowing or are sensitive to needles. 54. **ADEs associated with 5-alpha reductase inhibitors** 5-alpha reductase inhibitors are indicated for BPH. Examples include finasteride and dusateride ADE\ Decreased libido\ Impotence\ Gynecomastia\ Orthostatic hypotension 55. **Mechanism of action of GnRH analogs** Reversible chemical orchiectomy or oophorectomy. So it will temporarily disrupt the function of the testes/ovaries. It will reduce the production of sex hormones by inhibiting the pituitary glands release of luteinizing hormone and follicle stimulating hormone 56. **Anti-estrogen prevents osteoporosis** Raloxifene (Evista) prevention of osteoporosis, Post menopausal only 57. Which estrogen has the best estrogen when taken orally Estradiol has first-pass metabolism 58. **Medication interferes with progesterone used to terminate pregnancy** Mifeprisone\ RU486\ Terminates pregnancy\ Interferes with progesterone necessary to maintain pregnancy 59. **Contraceptive safe for use while breast feeding** **Intrauterine Devices (IUDs)**: Both hormonal and non-hormonal IUDs are safe and highly effective. Hormonal IUDs release progestin, which thickens cervical mucus to prevent sperm from reaching the egg1. It\'s important to avoid contraceptives containing estrogen, such as combined oral contraceptives, during the first few weeks postpartum, as they can affect milk supply