Pharmacy School

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  1. Drug-induced parkinsonism
    • Up to 20% of cases
    • Deplete dopamine: antiemetics (prochlorperazine) and antihypertensives (reserpine, methyldopa)
    • Block dopamine: certain antipsychotics, GI stimulants (metoclopramide)
    • Unknown mechanism: amiodarone, valproic acid, lithium
  2. Pramipexole
    • Mirapex
    • Dopamine agonist (non-ergot)
    • Elimination: renal tubule secretion
    • cimetidine increases half-life by 40%
    • For all dopamine agonists: adverse effects are often dose limiting, start low and go slow to limit ADEs, adverse effects similiar to levodopa except that DA agonists have increased somnolence, sleep attacks, and psychosis, decreased dyskinesia, increased impulse control disorders
  3. Ropinirole
    • Requip
    • Dopamine agonist (non-ergot)
    • Metabolism: CYP1A2 (remember, pramipexole is renal tubule secretion)
    • Drug inxs: CYP1A2 inhibitors like cipro, fluvoxamine, mexilitene
  4. Apomorphine
    • Apokyn
    • Dopamine agonist (non-ergot)
    • Rescue treatment of "off episodes in advanced PD as adjunct
    • onset: 10-20 minutes
    • duration: 60 minutes
    • contraindications: serotonin receptor antagonists coadministration will cause severe hypotension/loss of consciousness
    • Administer with Tigan to control N/V
  5. Bromocriptine
    Dopamine agonist (ergot derivative)
  6. Carbidopa/Levodopa
    • Sinemet
    • Levodopa converted to dopamine via DOPA decarboxylase which is inhibited by carbidopa in periphery
    • Side effects: stimulation of dopamine receptors in periphery leading to N/V, postural hypotension, cardiac arrhythmias, stimulation of dopamine receptors in CNS leading to hallucinations, also somnlence and dyskinesias and motor fluctuations (on and off periods)
    • Counseling tips:
    • o Take this medicine on an empty stomach at least 1 hour before or 2 hours after eating. If nausea or vomiting occurs, then may take with a snack.
    • o This medicine may cause dizziness, lightheadedness, or fainting. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.
    • o A dark color (red, brown, or black) may appear in your saliva, urine, or sweat after taking this medicine. This is not
    • harmful.
    • o The effects of this medicine might start to wear off between doses over time. Talk with your doctor if this medicine stops working well or if your condition worsens.
  7. Dopamine agonists Counseling tips
    • May cause nausea/vomiting
    • May cause somnolence and the possibility of falling asleep while engaged in activities of daily living. Do not drive or perform other possibly unsafe tasks until you know how you react to it.
    • This medicine may cause hallucinations (unreal visions, sounds, or sensations). Notify your doctor if this occurs.
    • This medicine may cause dizziness, lightheadedness,
    • or fainting; alcohol, hot weather, or exercise, may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects.
    • Hypotension and/or orthostatic symptoms may occur
    • more frequently during initial therapy or with an increase in dose at any time.
  8. Entacapone
    • COMT inhibitor which prevents peripheral conversion of levodopa to 3O methyldopa, allows for decrease of levodopa dose
    • Exacerbates all adverse events of levodopa (dyskinesias, nausea) if levodopa is not reduced
    • Also: urine discoloration, diarrhea
  9. Stalevo
    • carbidopa/levodopa/entacapone
    • Patient stable on IR C/L and entacapone separately, directly convert to stalevo
    • Stable on IR C/L but with wearing off, start entacapone and titrate to response before converting to stalevo
  10. Selegiline
    • Available genergic
    • Orally disintegrating (zelapar)
    • MAO-B inhibitor
    • Metabolized primarily by 3A4
    • Adverse events: nausea, dizziness, dry mouth
    • Transmucosal drug delivery significantly bypasses the gut and 1st pass metabolism
  11. Rasagiline
    • Azilect
    • MAO B inhibitor
    • Taken without regard to food
    • Metabolism 1A2
    • Adverse events: package insert includes dietary precautions similiar to MAO inhibitors (hypertensive crisis/chees reaction if patient ingests tyramine-rich foods although this is unlikely to happen)
    • Monotherapy: AEs similiar to placebo
    • Adjunct with levodopa: exacerbation of levodopa AEs
  12. Drugs to avoid with MAO-B inhibitors
    • Anti Ds: SSRIs, SNRIs, TCAs, mirtazapine?
    • Analgesics: meperidine, tramadol, methadon
    • Sympathomimetic amines: pseudoephedrine
    • Others: cyclobenzaprine, dextromethorphan, St. Jon's wort
  13. Amantadine
    weak antagonist of the NMDA type glutamate receptor, increases dopamine release, and blocks dopamine reuptake
  14. Dopamine agonist or levodopa as initial therapy for Parkinsons
    • Either levodopa or dopamine agonist can be used as initial therapy
    • DA are a good choice for younger patients since they are more likely to develop motor fluctuations on levodopa (taking for longer period of time)
    • Levodopa is often a better choice as initial therapy in older patients especially those who are cognitively impaired because of increased risk for psychosis/cognitive adverse effects with DA
  15. Neuroprotection?
    • No therapies recommended at this time
    • Not recommended: vitamin E, selegiline (MAO B inhibitor)
    • Insufficient evidence: pramipexole, ropinirole, coenzyme Q10
    • FDA committee rejected rasagiline as disease modifying agent for Parkinson disease
  16. Coenzyme Q10
    • Important for mitochondiral function, antioxidant
    • Available as dietary supplement, not standardized
    • Not recommended at this time
  17. Managing limitations of levodopa therapy: motor fluctuations
    • Wearing off, end of dose deterioration (Dietary protein may compete with transport of levodopa across gut and BBB, therefore timing of protein becomes more important with disease progression because of the loss of dopamine storage capacity of the neurons), increase frequency of carbidopa/levodopa, add COMT (entacapone) or MAO inhibitor (rasagiline) level A, add dopamine agonist (pramipexole or ropinirole) level B, May be considered Apomorpine, cabergline, selegiline (Level C), Should not be considered SR carbidopa/levodopa, bromocriptine (Level C)
    • On-off, freezing, unpredictable sudden change in PD control, unreleated to dose or timing
  18. Managing limitation of levodopa therapy: dyskinesias
    • Involuntary movement
    • Peak dyskinesias are most common: occur during "on" phase of drug therapy
    • Management: reduce levodopa dose and replace with dopamaine agonist, COMT inhibitor, MAO B inhibitor, or amantadine
  19. Parkinsons Disease: Management of adverse events: nausea
    • Take with food
    • Dopamine agonists: titrate slowly
    • Levo/carb - need at least 75-100 mg carbidopa to saturate DOPA decarboxylase (activation of peripheral dopamine receptors causes N/V)
    • Nausea usually subsides with continued use
    • Domperidone: peripheral dopamine antagonist, does not cross BBB, 30 minutes prior to carb/levo dose
  20. Parkinsons Disease: Management of adverse events: hallucinations/psychosis
    • Prevalence 20-40%
    • May be mild and not require treatment, may be related to medication or disease
    • If bothersome, 1st step is to reduce or stop stop drugs with least efficacy for PD symptoms or high risk for CNS adverse event (dopamine agonist)
    • anticholinergics, amantadine > selegiline > dopamine agonists >levodopa
    • Consider using atypicals (consider clozapine, may consider quetiapine, should not consider olanzapine because they can worsen motor symptoms)
  21. Parkinsons Disease: Management of adverse events: orthostatic hypotension
    • May be related to medication or disease
    • Intervention required for symptomatic OH
    • Interventions: reduce levodopa/dopamine agonist, increase salt intake, compression stockings, get up slowly; tilt head of bed, fludrocortisone (0.1mg up to 0.3 -0.9mg/d), midodrine 5 mg qd titrate to 10 mg BID
  22. Management of Acute Pancreatitis
    • Remove offending agent, if possible
    • Aggressive fluid and electrolyte repletion
    • Management of nausea and vomiting
    • Aggressive pain management
    • Nutrition support
    • Antimicrobials (not for prophylaxis)
    • Probiotics (not recommended)
    • Octreotide (use unclear)
  23. Management of Chronic Pancreatitis
    • 1. Abstain from alcohol, smoking cessation
    • 2. Treatment of malabsortion (pancreatic enzyme supplements, antacids, anti-secretory agents, possible reduction in fat intake)
    • 3. Relief from chronic pain (non-opioids, then try enzymes, then add opioids)
    • 4. Exogenous insulin
  24. Pancreatic Enzymes
    Use products that contain enzymes in small enteric-coated microspheres or mini-microspheres, administer with a meal or just after for mini-microspheres, products are NOT interchangeable, can give H2 blockers and PPIs at same time, Adverse effects (GI complaints, stricture or obstruction, fibrosing colonopathy, allergic-type reaction, hyperuricemia)
  25. Diabetic Neuropathy
    • Common complication of diabetes that can affect every tissue of the body.
    • Affects sensory, autonomic and motor neurons of the peripheral nervous system.
    • Responsible for the development of the diabetic foot syndrome and is associated with a reduced life expectancy.
    • Treatment:
    • TCAs: secondary amines (nortriptyline and desipramine) tolerated better than tertiary amines (amitriptyline and imipramine)--adverse effects (sedative, anticholinergic, orthostatic, cardiac, weight gain)
    • Gabapentin: equal effective to TCA with less side effects, adverse effects (somnolence, dizziness, confusion)
    • Pregabaline: FDA approved for PDN, mild to moderate dizziness, somnolence, and peripheral edema
    • Duloxetine: FDA approved for PDN, 1st line treatment along with TCAs, ADR (well tolerated, nausea most common, insomnia, dry mouth, constipation)
    • venlafaxine: not FDA approved for PDN, may cause cardiac arrhythmias
    • Topical: 5% lidocaine patch similiar level to pregabalin, capsaicin
    • Tramadol: Weak opioid μ receptor agonist and inhibits reuptake of serotonin and norepinephrine, ADRs (Dizziness,
    • nausea, constipation, somnolence, orthostatic hypotension, increased risk of seizures in patient with history of seizures or receiving other drugs that reduce seizure threshold, Elderly
    • Patients: cause or exacerbate cognitive impairment)
  26. Post-herpetic Neuralgia
    • Pain in the area affected by herpes zoster at least 3 months after crusting or rash, pain described as burning, aching, electric shock like pain or unbearable itching or steady, aching, boring pain.
    • Treatment:
    • Gabapentin: effective
    • Lidocaine patch—no more than 3 patches/12 hour period, then 12 hours off, adverse events: mild skin reactions, preferred for patients with focal neuropathy, shown to be at least as effective as pregabalin or gabapentin in open label studies
    • TCAs
    • Opioid analgesics: oxycodone or morphine
    • Pregabalin: effective
  27. Trigeminal Neuralgia
    • Idiopathic condition of severe, unilateral, paroxysmal facial pain
    • Brief episodes last from few seconds to longer than a minute
    • DOC: carbamazepine
    • Carb versus oxcarb: comparable analgesia, Oxcarbazepine: fewer adverse events including vertigo, dizziness, ataxia, fatigue but Increased incidence of hyponatremia
    • Refractory: Non-controlled studies with lamotrigine, topiramate, pregabalin and levetiracetam, have demonstrated
    • efficacy in refractory patients. Topiramate study had high drop-out rate due to adverse events
  28. Fibromyalgia
    • Unknown cause, widespread musclar pain, fatigue, and tenderness
    • Treatment: FDA approved drugs
    • Pregabalin: reduces and improves sleep and global measures
    • Duloxetine: SNRI, adverse effects: nausea, dry mouth, constipation, decreased appetite, somnolence, hyperhidrosis, agitation
    • Milnacipran: SNRI, ADRs, nausea, headache, constipation
  29. Treatment algorithm for ADHD
    • Stage 1: methylphenidate or amphetamine
    • Stage 2: stimulant not used in stage 1
    • Stage 3: atomoxetine
    • Stage 4: Bupropion or TCA
    • Stage 5: Bupropion or TCA not used in stage 4
    • Stage 6: alpha agonist (clonidine or guanfacine)
  30. ADHD meds: short acting, immediate release (4)
    • Methylphenidate (Ritalin®)
    • Dexmethylphenidate (Focalin®)
    • Mixed amphetamine salts (Adderall®)
    • Dextroamphetamine (Dexedrine®)
  31. ADHD meds: intermediate acting, sustained or extended release (2)
    • Methylphenidate (Ritalin-SR®)
    • Dextroamphetamine (Dexedrine Spansules®)
  32. ADHD meds: long acting, once daily (4)
    • Lisdexamfetamine (Vyvanse®)
    • Methylphenidate (Ritalin-SR®, Concerta®, Daytrana®)
    • Mixed amphetamine salts (Adderall XR®)
    • Dexmethylphenidate (Focalin XR®)
    • Metadate CD, Ritalin LA, Focalin XR (all extended release methylphenidate)—capsules may be opened (swallowing problems), less chance of insomnia, less chance of evening meal anorexia
    • Daytrana—transdermal patch for compliance issues
    • Lisdexamfetamine (Vyvanse)--Inactive prodrug in which d-amphetamine is bonded to l-lysine, Hydrolyzed in body to d-amphetamine, Less abuse (no “snorting”), Long acting
  33. Stimulant side effects and monitoring
    • Appetite loss (give after or during a meal, rather than before)
    • Insomnia (usually responsive to timing of last dose)
    • Abdominal pain and headache (probably will respond to taking medication with food
    • Agitation
    • Tics (not contraindication to taking stimulants)
    • Growth suppression (kids usually catch up)
    • CV risk--one study did not find an association, monitor BP, pulse rate, medical history (arrhythmias, cardiac anomalies, palpitation hx, hx of chest pain, history of fainting)
    • Monitor for side effects: at all visits (blood pressure, pulse, weight, height), check Appetite, headache, abdominal pain, sleep, tics, mood changes, irritability, most side effects responsive to changes in dose or timing
  34. Atomoxetine
    • Strattera
    • NERI--norepinephrine reuptake inhibitor, increased dopamine in prefrontal cortex
    • Stage 3 for ADHD
    • 2D6 metabolized
    • Some QTc changes, 2 cases of liver tox, suicidal risk is low (may increase suicidal thoughts in youths)
    • Versus stimulants: atomoxetine has far fewer sleep problems, appetite changes are variable, longer duration, benefits in non-responders to stimulants, similar CV side effects, non-scheduled
  35. Clonidine/Guanfacine
    • Central alpha 2-adrenergic agonist for ADHD
    • Less effective than stimulants, atomoxetine, or bupropion
    • Most common side effects are dose-dependent: Sedation, Hypotension, Constipation
    • Reports of bradycardia, syncope, rebound hypertension, heart block, and sudden death
    • Dose titration
  36. Pharmacotherapy for Alzheimer's disease
    • Mild to moderate: Cholinesterase inhibitors
    • Donepezil (Aricept)
    • Rivastigmine (Exelon)
    • Galantamine (Razadyne)
    • Moderate to severe: Donepezil and
    • Memantine (Namenda)--NMDA receptor antagonist
  37. Donepezil
    • Aricept
    • Selective AChe inhibition
    • Metabolized by 2D6 and 3A4
    • Take with or without food
  38. Rivastigmine
    • Exelon
    • AChe and BChe inhibition
    • Hydrolyzed by esterases (not metabolized in liver)
    • Take with food (increase in bioavailability)
    • Transdermal: fewer GI adverse events than oral dosing (vomting, nausea, diarrhea)
  39. Galantamine
    • Razadyne
    • Selective AChe inhibition and stimulates presynaptic nicotinic receptor
    • Metabolized by 2D6 and 3A4
  40. Assessment of Cognition Tests in Alzheimer's disease
    • To assess cognition:
    • MMSE (mini-mental state examination) less than 24/30 dementia
    • CLOX drawing (draw a clock)
    • Mini-cog (draw a clock and recall 3 items)
    • To assess effectivenss of cholinesterase inhibitors:
    • ADAS-cog (Alzheimer's disease assessment scale, out of 70 points, high score worse, change of 4 clinically significant)
    • MMSE (mini-mental state examination)
    • Clinician assessment (CIBIC Clinician's interview based impression of change, 7 point scale, score of 4 indicates no change)
  41. Key points: Efficacy of cholinesterase inhibitors
    • Only modest effects on cognition (Clinicians assessment: 12%-15% significantly improved compared to placebo)
    • Functional status has not been consistently evaluated in studies; inconsistent findings (Probably stabilizes activities of daily living)
    • No differences in efficacy among agents
    • Donepezil usually preferred 1st line
    • Rivastigmine has least change for drug inxs but more GI adverse events with oral dosing compared with donepezil
  42. Adverse events of cholinesterase inhibitors: cholinergic stimulation
    • Donepezil, Rivastigmine, Galantamine
    • Nausea/vomiting, diarrhea, anorexia (mostly associated with riv), dizziness, dyspepsia, agitations
    • Precautions in patients with:
    • Bradycardia-caution in patients with sick sinus syndrome, monitor in patients on other meds that slow heart rate
    • Ulcers
    • COPD or astham
    • Exaggerate succinylcholine type muscle relaxants during anesthesia
  43. Counseling tips: Cholinesterase inhibitors
    • May cause N/V
    • Take with meals to limit GI effects
    • Monitor for changes in appetite and weight (anorexia)
    • More likely to maintain current level of cognition and function rather than observe improvements
    • Do not interrupt therapy without prescriber advice
  44. Memantine
    • Namenda
    • NMDA antagonist
    • Primarily excreted unchanged in the urine, minimal CYP450 metabolism (rivastigmine also not metabolized by CYP450, primarily by esterases)
    • Use cautiosuly with other NMDA antagonists (amantadine in Parkinson's, dextromethorphan, ketamine) and other medications eliminated via tubular secretion
    • Efficacy: add on to donepexil therapy, probably more beneft with both than just donepezil
  45. Efficacy: other agents for treating Alzheimer's disease
    • estrogen, vitamin D, anti-inflammatory agents--no evidence for prevention or treatment
    • Ginkgo Biloba-natural supplement, generally not recommended for treatment
  46. Behavioral and Psychological Symptoms of Dementia (BPSD)
    • No medications are approved to treat BPSD
    • Atypical antipsychotics (remember that clozapine and olanzapine have anticholinergic effects)
    • Antidepressants (avoid TCAs, paroxetine because of long half-life)
    • Avoid benzos
    • Carbamazepine may be useful, valproic not effective in trials
    • For:
    • Psychosis: atypicals
    • Aggression or agitation: mild (mood stabilizers, antidepressants, buspirone) severe (atypicals)
    • Disturbed mood or affect: antidepressants
    • Atypicals and CV risk--increased risk for cerebrovascular adverse events with trials for risperidone and olanzapine, 50-70% increase in mortality
    • Cholinesterase inhibitors may have small benefit on neuropsychiatric symptoms but not recommended as treatment for BPSD alone
  47. 17 beta estradiol
    • Biological estrogen
    • Most potent endogenous activator of estrogen receptors
    • 95% produced by ovaries
    • After menopuase, produced by estrone from liver and adipose tissues
    • 12x more potent than estrone, 80x more potent than estriol
    • Oral, transdermal and vaginal products
    • Oral administered products undergo metabolism in liver resulting in high levels of estrone and low amounts of estradiol
    • Transdermal and vaginal products by-pass first gut/liver metabolism (transderal 20x higher than oral)
  48. Estrone
    • Biological estrogen
    • 50% produced by ovaries
    • Procuced from estradiol and estrone sulfate
    • Also produced by liver and adipose tissues
  49. Conjugated estrogen extracts CEE
    • Premarin
    • Contains at least 10 estrogens as sulfate esters including estradiol sulfate and estrgone sulfate, all 10 are biologically active and have potent estrogenic effects
  50. Estrogen in menopause: adverse effects
    • Common: nausea, headache, breast tenderness, heavy bleeding
    • Serious: coronary heart disease, stroke, venous thromboembolism, breast cancer, gallbladder disease
  51. Transdermal versus oral estrogens: risks and benefits
    CEE versus oral estradiol: risks and benefits
    • 17 beta estradiol doses are significantly lower than non-oral routes due to by-passing first pass liver metabolism
    • Oral doses: need 1-2 mg/day of oral estradiol to reduce hot flashes and help with sleep
    • Transdermal doses: require much lower doses to get same effect
    • Oral, but not transdermal estradiol is associated with an increased risk of thromboembolism.
    • CEE (conjugated estrogen extract) but not oral estradiol resulted in an increased risk of thromboembolism.
    • So, conjugated estrogen extract associated with more clot risk than oral estradiol, and oral estradiol associated with more clot risk than transdermal—patch is probably safest
    • Large observational study found similar risk for breast cancer for both oral and transdermal estrogens
  52. Progestogens in treating menopause
    • Used to protect uterus against the increased risk of endometrial hyperplasia and cancer with estrogen monotherapy. (progestin not needed if there is no uterus)
    • A minimum of 12-14 days of progestogen therapy is needed; however continuous therapy is commonly used.
    • If you do not use continuous progestogens, withdrawal bleeding occurs. No physiological need for monthly
    • bleeding.
  53. Medroxyprogesterone MPA for menopause
    • Combination product with CEE
    • Also used in Depo provera
    • Significant anti-estrogenic effects
    • Store in a closed container at room temperature, away from heat, moisture, and direct light
  54. Progesterone (micronized) in menopause
    • Endogenous progestin that is most potent activator of progesterone receptor
    • Administration with food increased peak levels and AUC
    • CI: Allergy to peanuts; contains peanut oil (oral)
    • Store in a closed container at room temperature, away from heat, moisture, and direct light.
    • Adverse effects: drowsiness, dizziness. Take at bedtime if needed.
  55. Norethindrone acetate for menopause
    • Combined estrogen-progestagen oral and dermal patch products
    • Only progestin in combined dermal patch with estradiol
  56. Side effects of HRT
    Nausea, breast tenderness and pain, endometrial stimulation, withdrawal bleeding, headache, weight gain, transdermal: skin irritation, erythema, rash
  57. Menopause clinical studies
    • Nurses Health Study: increased risk breast cancer, increased risk ischemic stroke, no change in fatal cardiovascular disease risk, possible protective effect against coronary disease
    • Women's Health Initiative: estrogen only study stopped early due to increased risk of stroke, estrogen only for 7 years found no increased risk of breast cancer, combined estrogen + progestin therapy increases risk of breast cancer, found no CV protective effect, found increase in stroke and DVTs, and PE, higher percent of WHI women were older and more obese
    • HERS: Heart and Estrogen replacement therapy: HRT possibly harmful to older women with advance arterial disease, some studies suggest that younger women are at lower risk of HRT-associated CHD
  58. Vasomotor Symptom Risk Factors
    • Obesity increases risk of hot flashes, smoking increases risk, ethnicity (African Americans and latino greater than caucasians greater than asians
    • Higher the intensity of hot flashes, the lower the risk of breast cancer
  59. Vasomotor symptoms: treatment
    • Estrogens: most effective, lower doses associated with fewer side effects (uterine bleeding, breast tenderness)
    • With hysterectomy, don't need to give progestin
    • On-off treatment of concern: 1st treatment possibly has greatest risk of blood clots
    • Bioidential hormones: not natural estrogens, never recommend
    • SSRIs, SNRIs, and gabapentin: mixed results
    • Phytoestrogens: possible benefit but also increased risk of endometrial hyperplasia
    • Black cohosh: GI complaints, rashes, rare liver tox
  60. Vaginal symptoms of menopause: treatment
    • Includes dryness, discomfort, itching and dyspareunia
    • Vaginal estrogens: typicall progestin therapy not prescribed
    • Side effects: vaginal irritation, itching, burning, parathesia (report any vaginal bleeding)
  61. Urogenital symptoms of menopause: treatment
    • Estrogen used vaginally or systemically reduces the symptoms of overactive bladder.
    • Vaginal estrogen reduces the incidence of recurrent urinary tract infections.
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Pharmacy School
2012-05-07 06:59:29
Midterm Information

Everything for midterm 2
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