Drugs Flashcards

Question

Scopolamine

Answer 1

=anticholinergic agent, antiemetic -as a transdermal patch MoA: blocks ACh (M) receptors in the CTZ, vestibular nuclei, and in the GI tract Adverse rxns: -sedation, blurred vision (crosses BBB), reduced GI and bladder tone Therapeutic use: motion sickness

Answer 2

Antihistaminic agent, antiemetic, Ethanolamine derivative =dramamine -widely used in motion sickness and effective because of anticholinergic action Adverse rxn: sedation, blurred vision, dry mouth Therapeutic uses: -motion sickness, mild n/v

Answer 3

=1st generation Piperazine derivative -antiemetic, antihistamine agent -use of these agents during pregnancy remains controversial despite no increase in the incidence of birth defects in several large prospective trials Therapeutic use: vertigo, motion sickness -effective because of anticholinergic action

Answer 4

=1st generation Piperazine derivative -antiemetic, antihistamine agent -use of these agents during pregnancy remains controversial despite no increase in the incidence of birth defects in several large prospective trials Therapeutic use: vertigo, motion sickness -effective because of anticholinergic action

Answer 5

-antiemetic, blocker of serotonin receptor (5-HT3 subtype) -for IV and oral use MoA: selectively blocks serotonin receptors in the GI tract and in the CTZ PK: metabolized by P450 enzymes but does not induce or inhibit them (potential for DI) Adverse reactions: -headache, diarrhea, constipation, asthenia, and phlebitis -hypersensitivity reactions (rare) -ECG changes (QT interval prolongation) (rare) Advantages: -these drugs do not produce extrapyramidal side effects Therapeutic uses: -post-op n/v following highly emetogenic surgical procedures -n/v due to administration of highly and moderately emetogenic agents (nitrous oxide, ketamine, opioids, antineoplastics) -radiotherapy-induced n/v -NOT effective against motion sickness -can be used for kids ages 4-11

Answer 6

-antiemetic, blocker of serotonin receptor (5-HT3 subtype) -for IV and oral use MoA: selectively blocks serotonin receptors in the GI tract and in the CTZ PK: metabolized by P450 enzymes but does not induce or inhibit them (potential for DI) Adverse reactions: -headache, diarrhea, constipation, asthenia, and phlebitis -hypersensitivity reactions (rare) -ECG changes (QT interval prolongation) (rare) Advantages: -these drugs do not produce extrapyramidal side effects Therapeutic uses: -post-op n/v following highly emetogenic surgical procedures -n/v due to administration of highly and moderately emetogenic agents (nitrous oxide, ketamine, opioids, antineoplastics) -radiotherapy-induced n/v -NOT effective against motion sickness

Answer 7

capsules =Neurokinin-1 receptor antagonist, antiemetic MoA: selective, high affinity antagonist of neurokinin 1 (NK1) receptors Drug interactions: a potent inhibitor of CYP3A4 Therapeutic uses: -in combination with other antiemetics for acute and delayed n/v due to initial and repeat courses of highly emetogenic antineoplastic drugs **especially useful for delayed vomiting

Answer 8

for tx of n/v -chemically synthesized delta-9-tetrahydrocannabinol -Schedule II drug -"medical marijuana" MoA: unknown, binds to receptors in CTZ, vomiting center, and cortex Caution: impairs cognitive and motor performance and may induce dysphoria and psychotomimetic behavior Therapeutic uses: -n/v due to use of highly emetogenic antineoplastic drugs -anorexia associated with weight loss in AIDS patients

Answer 9

-glucocorticoids, antiemetics MoA: inhibits the synthesis of proinflammatory PG's in the CNS, thereby blocking cortical projections to the emetic center Therapeutic uses: -given IV as adjunct therapy with other antiemetics with highly emetogenic agents

Answer 10

Benzodiazepines, antiemetics | Therapeutic uses: n/v due to emotional factors (anticipatory n/v)

Answer 11

-for migraine that causes mild to moderate disability -ideal drug for women who are pregnant (risk factor B) CI: severe liver and kidney disease and G6P deficiency disease

Answer 12

nonsteroidal antiinflammatory drug | for migraine that causes mild to moderate diability

Answer 13

nonsteroidal antiinflammatory drug | for migraine that causes mild to moderate diability

Answer 14

nonsteroidal antiinflammatory drug for migraine that causes mild to moderate diability -useful to treat n/v and enhance gastric absorption

Answer 15

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -effective during the actual migraine attack, but not during the aura

Answer 16

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -metabolized principally by the A isoenzyme of monoamine oxidase and the metabolites are excreted in the urine PK may be altered in severe liver impairment

Answer 17

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -only available as an oral tablet -excreted largely as unchanged drug in the urine, kinetics may be altered in renal impairment

Answer 18

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -metabolized principally by the A isoenzyme of monoamine oxidase and the metabolites are excreted in the urine -no dose adjustment is required in the elderly or in patients with renal or hepatic impairment

Answer 19

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -available only as an oral tablet -metabolized by one minor and 2 major pathways MAO-mediated oxidative deamination and cytochrome P450-mediated oxidation are the major routes -flavin monooxygenase is the minor route

Answer 20

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -available only as oral tablet

Answer 21

serotonin agonist -med for migraine causing moderate to severe disability -5-HT1B/1D agonists 1B is restricted to intracranial blood vessels 1D and 1F are located on neurons -if attack is not aborted with one dose, or with a subsequent dose given 2-4 hours later, it is unlikely that the med will help the attack CI: documented or ischemic heart disease, hx of MI, silent ischemia, Prinzmetal's angina, uncontrolled HTN and suspected CAD -not for management of basilar of hemiplegic migraine -should not be taken concurrently or within 24 hours of ergots or other triptan agents -available only as an oral tablet -primarily metabolized by CYP450 and CYP3A4

Answer 22

- oldest serotonergic receptor agonist - less selective than the triptans - ergotamine tartrate has poor and erratic GI absorption, relatively common side effects, and frequent habituation - prolonged use leads to ergotism and/or rebound headache - avoid prolonged administration of excessive dosage due to danger of ergotism and gangrene - because of long duration of effect, the drug should be used no more than every 4th day, or 2x/week

Answer 23

DHE probably does not produce drug-induced headache - serotonin receptor agonist - med for migraine causing moderate to severe disability - can use IV DHE for intractable migraine or status migrainosus - use with caution in pt with hypertension, angina, peripheral vascular disease, and impaired renal and hepatic function - avoid in pregnancy - patients who have liver impairment need lower doses - when used with heparin, the usual cautions and contraindications for heparin as well as DHE must be followed

Answer 24

includes: - Prochlorperazine - Chlorpromazine - Droperidol - proved effective in treating migraine attacks, particularly when patients have prolonged migraine (status migrainosus) and significant n/v

Answer 25

- for patients who have infrequent, moderate to severe headaches that do not respond to standard medication - particularly useful for patients who cannot use specific headache meds because of coexisting disease or lack of dx - safe treatment for pregnant women when given in limited amounts

Answer 26

includes: -propanolol -timolol -these 2 are FDA approved for migraine prophylaxis -patients with inadequate myocardial function, acute withdrawal may exacerbate sx Caution in patients with bronchospastic disease, hyperthyroidism, impaired liver function -drug should be withdrawn over 1-2 weeks -may potentiate hypoglycemia in diabetic patients Adverse rxns: -depression, tiredness, weakness, dizziness, wheezing, irregular heart beat, decreased sexual activity and bradycardia -lethargy is most likely with propanolol -BB without intrinsic sympathomimetic activity are effective

Answer 27

Verapamil and Flunarizine -used in migraine prevention Caution: -verapamil has significant inhibitory effects on cardiac conduction system and is considered a class IV antiarrhythmic agent -use with caution in renally or hepatically impaired patients -use with caution in patients with CHF

Answer 28

anti-epileptic - used for migraines - GABA agonist - discontinue if pt has abnormal liver function tests - pregnancy risk factor D

Answer 29

anti-epileptic drug, FDA approved for migraines | -sulfamate substituted monosaccharide with action at GABA-A and nonNMDA receptors

Answer 30

-older anti-epileptic drug 90% protein bound in serum -free fraction of drug is responsible for therapeutic effect -interact with other drugs that are highly protein bound MoA: produces voltage- and frequency-dependent block of Na channels --> prevents high-frequency action potentials but allows firing at more typical frequencies -effective for partial and GTC seizures, but not for myoclonic, atonic, or absence sz -has non-linear pharmacokinetics -induces hepatic CYP450 enzymes, and high protein binding -half-life gets longer with higher doses -IV solution is mixed with propylene glycol and ethanol as diluents, can cause hypotension and cardiac arrhythmias -thrombophlebitis and "purple glove syndrome" may also occur Side effects: -sedation -imbalance -diplopia -dizziness -gingival hyperplasia -hirsutism -acne -coarsening of facial features -hepatotoxicity -myelosuppression -rash (sometimes serious) *drug that works primarily on Na channels

Answer 31

antiepileptic drug *drug that works primarily on Na channels has a tricyclic ring structure -blocks Na channels in a frequency- and voltage-sensitive manner similar to that of phenytoin -effective for partial and GTC seizures **often makes absence, atonic, and myoclonic seizures worse -acute and dangerous side effects similar to phenytoin, but none of the cosmetic side effects -also produces hyponatremia -dose dependent decreases in WBC count common -major hepatic inducer, induces its own metabolism -has epoxide metabolite that may be responsible for some of the toxic side effects -can cause Stevens-Johnson syndrome -found that among several Asian populations, this reaction is very highly correlated with the presence of HLA haplotype (HLA B*1502) --> need to be HLA typed before getting the drug

Answer 32

*drug that works primarily on Na channels -antiepileptic drug = slight modification of the molecule that doesn't have the epoxide metabolite --> works the same way but is better tolerated -it's converted to monohydroxyderivative (MHD), which has the actual antiepileptic action -does not induce hepatic enzymes -no hepatic or hematologic toxicity -hyponatremia is a little more common and more prominent -MHD metabolite is renally excreted

Answer 33

-antiepileptic drug *drug that works primarily on Na channels MoA: enhances the slow inactivated state of the channel -must have additional moa's because it is a broad spectrum drug with efficacy against all seizure types Side Effects: -ataxia, diplopia, dizziness are rare -most common side effects are headache, insomnia, and rash -no liver/blood toxicity -levels are decreased by hepatic inducers and doubled by concurrent valproic acid *may be drug of choice for women with epilepsy who want to get pregnant

Answer 34

*drug that works primarily on Na channels antiepileptic -works by enhancing slow inactivation of the Na channel, which is a different mechanism from the fast inactivation that is enhanced by the other drugs -seems to cause synergistic toxicity when given with other Na channel drugs -very new, needs more data

Answer 35

antiepileptic *drug that works on GABAergic system Lorazepam and Diazepam = tx of choice for acute seizures Midazolam = extremely short acting, used as an IV drip for refractory status epilepticus Clonazepam = used for chronic tx, not beneficial except for myoclonic seizures --> benzos lose effects with chronic use and can be addictive -effective in the short term for all seizure types -cause sedation and respiratory depression (oral doses never lethal unless taken with as a combo with other sedatives) -bind to allosteric modulation site on GABA-A receptor -receptor is coulpled to Cl- channel, channel opens more frequently --> hyperpolarization and greater inhibition

Answer 36

= a competitive antagonist of the benzodiazepine receptor and may produce seizures in patients taking benzos

Answer 37

antiepileptic *drug that works on GABAergic system = Barbiturate -half life of 96 hours -bind to an allosteric modulation site on GABA-A receptor that is different from the one used by benzos -binding to this site causes the associated Cl- channel to remain open longer each time that it opens --> increased Cl- hyperpolarizes the cell and tends to impede its firing -does not produce tolerance with chronic use the way benzos do -IV barbs causes sedation and significant respiratory depression -orally --> produce sedation, depression, and cognitive impairment -can induce hepatotoxicity and allergic rashes -overall lousy drugs, should only be used in infants (they don't absorb anything else well enough), for status epilepticus, or for very economically disadvantaged patients (pennies per dose)

Answer 38

``` antiepileptic *drug that works on GABAergic system -works as selective GABA reuptake inhibitor -used only for partial seizures -in people with generalized epilepsy can cause absence status epilepticus, presumably due to its effects on the GABAergic synapses in the reticular nucleus of the thalamus Side effects: -sedation -cognitive impairment -depression ```

Answer 39

-antiepileptic -drug that acts on T-type calcium channels -blocks the "transient" (T-type) calcium channels in the thalamus in a voltage-dependent manner --> appears to stop abnormal thalamic excitability without inhibiting normal activity -prevents development of cortico-thalamic interactions which underlie the 3 Hz spike-and-wave of absence seizures -no efficacy against any other seizure type Side effects: -sedation, dizziness, cognitive impairment, headache, and behavioral changes -rashes and myelosuppression are medically dangerous issues

Answer 40

- antiepileptic * drug with multiple putative mechanisms of action - works against all seizure types (may be a bit less effective than carbamazepine against partial seizures) - many different pharm effects: 1) increases in synaptic GABA 2) attenuation of excitatory activity mediated by NMDA-type glutamate receptors 3) reduction of sustained repetitive firing of neurons - significant inhibition of hepatic CYP450 enzymes and very high protein binding - produces GI upset (koted Depakene) - sedation, cognitive impairment - also: weight gain, hair loss, tremor - hepatic failure - dose dependent thrombocytopenia, pancreatitis - reversible form of polycystic ovary syndrome in many women - AED most firmly linked with teratogenicity (neural tube defects in 2% of infants)

Answer 41

-antiepileptic -drug with multiple putative mechanisms of action -efficacy against all seizure types except absence seizures MoAs: 1. inhibition of voltage-sensitive Ca channels in hippocampus 2. enhancement of GABA-induced Cl- currents 3. inhibition of AMPA/kainate type glutamate receptors 4. inhibition of carbonic anhydrase -very safe drug -nephrolithiasis in 1% due to CA inhibition -very rare cases of reversible acute angle-closure glaucoma Dose related side effects: -paresthesias, sedation, cognitive impairment -can be potent but are transient -weight loss -also works for migraines, pain, and essential tremor

Answer 42

-antiepileptic -drug with multiple putative mechanisms of action -broad spectrum drug, efficacy against all seizure types -phenytoin-like effects on Na channels -ethosuximide-like effects on Ca channels -carbonic anhydrase inhibition Side effects: -sedation, dizziness, cognitive impairment -decreased appetite -rashes, kidney stones (1%) -very rare agranulocytosis -oligohydrosis with hyperthermia

Answer 43

-antiepileptic -drug with unique MoA -no effect on Na or Ca channels, GABA, or glutamate -drug binds very strongly and specifically to synaptic vesicle protein SV2A (don't know what it does) Side effects: -sedation, irritability, psychosis (1%)

Answer 44

-antiepileptic -drug with unique MoA -designed as a GABA-analog, but it's NOT! --> its actions appear to have little or nor relation to GABAergic neurotransmission -as effective for tx of chronic pain as it is for epilepsy -drug is now used far more for pain than for seizures -only effective for partial seizures -limited by gastric absorption (prompted development of pregabalin) Side effects: -sedation and weight gain -elimination is entirely renal

Answer 45

- penicillins/cephalosporins - sulfonamides - aminoglycosides - fluoroquinolones * **use in contact lens wearers for Pseudomonas coverage (contacts make pt more prone to Pseudomonas infection)

Answer 46

- non-steroids (worsen herpes, NSAIDs have been associated with corneal melting) - corticosteroids --> can cause cataracts, glaucoma, delay wound healing

Answer 47

intraocular pressure lowering agent ("ocular anti-hypertensive") purple cap MoA: activation of alpha-2 receptors in ciliary body inhibits aqueous secretion Side effects: Local --> irritation, allergy, mydriasis Systemic --> dry mouth, hypotension, lethargy CI: MAO inhibitor use, Brimonidine (Alphagan) is not to be used in children younger than 2 years, associated with apnea in kids

Answer 48

intraocular pressure lowering agent ("ocular anti-hypertensive") eg Timoptic (= Timolol maleate) MoA: blockade of beta-receptors in the ciliary body reduces intraocular pressure by decreasing aqueous humor production Side Effects: Local --> blurred vision, corneal anesthesia, superficial punctate keratitis Systemic --> bradycardia/heart block, bronchospasm, fatigue, depression, impotence, decreases sensitivity to hypoglycemic sx in insulin dependent diabetics, worsening myasthenia gravis CI: asthma, severe COPD, bradycardia, heart block, CHF, myasthenia gravis

Answer 49

intraocular pressure lowering agent ("ocular anti-hypertensive") MoA: inhibition of enzyme carbonic anhydrase decreases aqueous production in ciliary body -when given parentally, CAIs will also dehydrate the vitreous Side effects: local, drops --> eg Trusopt = Dorzolamide hydrochloride, bitter taste systemic, drops --> diuresis, fatigue, GI upset, Stevens-Johnson, theoretical risk of aplastic anemia systemic with oral or IV (diamox = acetazolamide) --> hypokalemis/acidosis, renal stones, paresthesias, nausea, cramps, diarrhea, malaise, lethargy, depression, impotence, unpleasant taste, aplastic anemia, Stevens-Johnson CI: sulfa allergy, hypo-natremia/-kalemia, recent renal stones, thiazide diuretics, digitalis use

Answer 50

intraocular pressure lowering agent ("ocular anti-hypertensive") MoA: dehydrates the vitreous and decreases intraocular fluid volume by osmotically drawing fluid into the intravascular space, given orally or IV Side effects: mannitol --> CHF, urinary retention in men, back ache, MI, headache, mental confusion glycerin --> vomiting, less likely to produce CHF than mannitol, otherwise similar to mannitol isosorbide --> same as glycerin except safer in diabetes CI: CHF, diabetic ketoacidosis (glycerin), subdural or subarachnoid hemorrhage, pre-existing severe dehydration

Answer 51

intraocular pressure lowering agent ("ocular anti-hypertensive") MoA: direct cholinergics (pilopine HS = pilocarpine) stimulate muscarinic receptors and indirect cholinergics (phospholine iodide = echothiophate iodide) block acetylcholinesterase -miotics cause pupillary muscle constriction, believed to pull open the trabecular meshwork to increase trabecular outflow Side effects: direct cholinergic: local --> brow ache, breakdown of blood/aqueous barrier, angle closure (increases pupillary block and causes the lens/iris diaphragm to move anteriorly), decreased night vision, variable myopia, retinal tear/detachment, and possibly anterior subcapsular cataracts systemic --> rare CI: peripheral retinal pathology, central media opacity, young patient (increases myopic effect), uveitis Indirect cholinergic: local --> retinal detachment, cataract, myopia, intense miosis, angle closure, increase bleeding post surgery, punctal stenosis, increase formation of posterior synechiae in chronic uveitis systemic --> diarrhea, abdominal cramps, enuresis, increases effect of succinylcholine CI: succinylcholine administration, predisposition to retinal tear, anterior subcapsular cataract, ocular surgery, uveitis

Answer 52

intraocular pressure lowering agent ("ocular anti-hypertensive") eg Xalatan = Latanoprost MoA: Prostaglandin F-2alpha analogues increase uveoscleral outflow by increasing extracellular matrix turnover in the ciliary body face Side Effects: local --> increase melanin pigmentation in iris, blurred vision, eyelid redness, cystoid macular edema and anterior uveitis, hypertrichosis (long lashes) systemic --> systemic upper respiratory infection sx, backache, chest pain, myalgia CI: pregnancy, inflammatory conditions

Answer 53

intraocular pressure lowering agent ("ocular anti-hypertensive") (eg Propine = Dipivefrin) MoA: in the ciliary body, the response is variable (beta stimulation increases aqueous production, but alpha stimulation decreases aqueous production) -in the trabecular meshwork, beta stimulation causes increased trabecular outflow and increased uveoscleral outflow -overall effect is IOP lowering Side effects: local --> cystoid macular edema in aphakia (more likely with epinephrine than dipivefrin), mydriasis, rebound hyperemia, blurred vision, adenochrome deposits, and allergic blepharoconjunctivitis systemic --> tachycardia/ectopy, hypertension, headache CI: narrow angles, aphakia, pseudophakia, soft lenses, hypertension, cardiac disease

Answer 54

the iris contains the iris dilator and constrictor muscles. The sphincter muscle and circular muscle in the ciliary body control accommodation and are innervated by the parasympathetic system -iris dilatory muscle is innervated by sympathetic system -Parasympatholytic agents (mydriacyl = tropicamide, atropisol = atropine sulfate) -block acetylcholine receptors in iris sphincter and ciliary body causing mydriasis and cycloplegia -Sympathomimetic agents (mydfrin = phenylephrine) -stimulate the dilator muscle causing mydriasis Side effects and CIs noted previously

Answer 55

-mood stabilizer =excellent, inexpensive medication, effective treatment for bipolar disorder MoA: not known, might act differently on different parts of the brain Uses: -better for treating mania than depression of bipolar disorder, but can be used for both -enhance the effect of antidepressants in patients with major depressive episodes Side effects: -tremor -polyuria/polydipsia -weight gain -cognitive slowing -hypothyroidism -decrease renal function*** -derm (acne) -memory problems -n/v, diarrhea Pregnancy category D, avoid in 1st trimester because of Ebstein's abnormality Overdose: lethal in blood levels about 3.0 mEq/L, toxic above 1.5 -sudden discontinuation associated with risk of relapse (taper over 3 months) -many drug interactions Food interactions: -caffeine decreases levels -green tea decreases levels -narrow therapeutic window, requires monitoring of plasma drug levels Toxicity: -coarse tremor, muscle fasciculations, confusion or stupor, slurred speech, ataxia, vomiting, arrhythmia, seizures **monitor kidney function (where it is excreted) -Monitor TSH as Li can result in hypothyroidism

Answer 56

anticonvulsant as mood stabilizer -anticonvulsants augment the synthesis and release of GABA and inhibit its reuptake and breakdown, affect glutamate by reducing its release MoA: interferes with Ca and Na channels and thus enhances GABA and inhibits glutamate Efficacy: -acute mania -bipolar prophylaxis (may be effective) -mixed, rapid-cycling bipolar -seizure disorders Side effects: -weight gain -sedation -GI upset -dizziness -hair loss -associated with polycystic ovaries *pancreatitis *hepatitis *thrombocytopenia Pregnancy category D (increased risk of neural tube defects) Overdose: serious effects notable mostly at 20 times the normal serum level -rapid discontinuation increases the risk of rapid relapse in bipolar disorder Drugs that increase valproate serum levels: CAFE PI Drugs that reduce valproate serum levels: CREPes Drugs whose metabolism is inhibited by valproate: i sAW LAND

Answer 57

anticonvulsant as a mood stabilizer MoA: act on Na and K channels to enhance GABA availability -not FDA approved but has been used longest for mood -not used as 1st line for bipolar because of effect on/interactions with other meds -often reserved for patients who fail other tx Efficacy: -acute mania -mixed, rapid-cycling bipolar -seizure disorders Side effects: -sedation -dizziness -fatigue, n/v, constipation, diarrhea *Thrombocytopenia and aplastic anemia *hepatitis *Stevens-Johnson --> test Asian people for HLA B1502 before prescribing this Overdose: serious sx occur at 10-20x normal serum levels Pregnancy Category D (congenital malformations -rapid discontinuation related to increased risk of relapse Drug interactions: "everything" -acetaminophen levels are decreased by carbamazepine but the risk for hepatotoxicity is increased with overdose *must have 14 day period washout before and MAOI is started (serotonin syndrome)

Answer 58

anticonvulsant as a mood stabilizer MoA: reduces the excitatory actions of glutamate via interference with Na channels Efficacy: great for bipolar depression and maintenance Side effects: -sedation -dizziness/ataxia/ decreased coordination -headache -n/v *Stevens-Johnson --> stop med for anyone who develops a rash Pregnancy category C: no controlled studies in pregnant women, avoid in 1st trimester Drug interactions: carbamazepine, valproate, phenytoin, phenobarbital -NONE with Li, CAN be used with MAOi

Answer 59

=typical antipsychotics MoA: -dopamine antagonists -competitively block dopamine receptors (D2, 3, and 4) -block D2 receptors 10-50 times more avidly than D3 -D2 receptors are located in limbic, extrapyramidal, and endocrine structures -D3 and D4 are located primarily in limbic structures Side effects: Extrapyramidal: -Parkinson syndrome -Acute dystonia -Tardive dyskinesia -Neuroleptic malignant syndrome -Akathisia Cardiovascular: -prolongation of QT Endocrine: -increased prolactin -amenorrhea Metabolic Syndrome: -increased risk of diabetes, stroke, and heart disease Anticholinergic properties (dry mouth, etc) Antihistaminergic (weight gain and sedation) alpha adrenergic blockade (orthostatic hypotension) Dopaminergic blockade (D2, results in EPS)

Answer 60

MoA: serotonin/dopamine antagonists -competitively block serotonin receptors (5-HT2 subtype) -cause a higher degree of binding to and blockade of D4 and D3 receptors rather than D2 receptors -have a 5 fold or greater binding affinity for serotonergic receptors than D2 receptors -5-HT2 receptors located in cortical structures where the negative symptoms of schizophrenia are though to originate -have a 10 fold or greater binding affinity for D4 receptors than D2 receptors -D4 and D3 located in limbic structures where the positive sx of schizophrenia are thought to originate -serotonin inhibits dopamine release in the frontal lobes and has small impact in the mesolimbic and nigrostriatal pathways, blockade of these receptors accomplishes: -improves the negative sx of schizophrenia -reduces the EPS side effect profile -improves the + sx MoA: dopamine agonist/antagonist -establishes balanced dopamine availability by serving as antagonist in areas with excessive dopamine (mesolimbic) and as agonist in areas with low dopamine (frontal lobes, nigrostriatal pathway) -currently only Aripiprazole (Abilify) is available Side effects: Extrapyramidal: -Parkinson syndrome -Acute dystonia -Tardive dyskinesia -Neuroleptic malignant syndrome -Akathisia Cardiovascular: -prolongation of QT Endocrine: -increased prolactin -amenorrhea Metabolic Syndrome: -increased risk of diabetes, stroke, and heart disease Anticholinergic properties (dry mouth, etc) Antihistaminergic (weight gain and sedation) alpha adrenergic blockade (orthostatic hypotension) Dopaminergic blockade (D2, results in EPS)

Answer 61