Medications/Pharm Flashcards
MOA of Valproic Acid
Valproic acid increases Na+ channel inactivation and increases GABA concentration by inhibiting GABA transaminase.
MAO of Carbidopa →
inhibits DOPA decarboxylase and thereby prevents the peripheral metabolism of levodopa to dopamine before it can cross the blood–brain barrier
Tobacco smoking is a potent inducer of ________
CYP 1A2
Which antipsychotic is a serotonin 1A agonist and also has SNRI properties
Ziprasidone
blockade of the 5-HT 1A receptor
Carbamazepine is inducer of CYP _____ and ____
- Carbamazepine is inducer of CYP 2C19 and 3A4
How does cabamazepine interact with lamotrigene?
- Carbamazepine is inducer of CYP 2C19 and 3A4
- does not affect clozapine levels (but don’t use it because agranulocytosis risk)
- Will decrease warfarin, alprazolam, propranolol, citalopram levels
- Lowers lamotrigine by induction of glucuronidation 1A4
*
Buspirone works on _________
- Buspirone works on serotonin 1A partial agonist
- Can increase haloperidol levels ; takes 2-3 weeks to work ; can’t use with MAOis
WHich AED lowers efficacy of OCPs the most?
AEDs have the warning for lower oral contraception efficacy ; carbamazepine lowers OCPs the mos
best TCA for childhood enuresis
Imipramine
Memantine MOA
- Memantine → antagonist of NMDA → slows Ca++ influx (halt cell destruction)
cholinesterase inhibitors
Tacrine, donepezil, galantamine, rivastigmine
Bupropion is a CYP ________ _______
Bupropion is a CYP 2D6 inhibitor
- selective for MAO-B
Selegeline
Metabolism of Paliperidone vs Risperidone
- Paliperidone goes through the kidneys (80%); risperidone goes through liver to become paliperidone
Lithium toxicity Levels
- Mild/mod ______ → ________________________
- Mild/mod 1.5-2.0 → vomiting, abdominal pain, ataxia, dizziness, slurred speech, dry mouth
Lithium Toxiity:
- Mod/severe ______ → ________________________
- Mod/severe 2.0-2.5 → anorexia, muscle fasciculations, clonus, increased DTRs, other movements, seizures, delirium, circulatory failure
*
Lithium Toxiity:
- Severe → ______ → ________________________
Severe >2.5 → seizures, oliguria, renal failure, death
Atomoxetine
- NE reuptake inhibitor for ADHD
- takes 10 weeks to take effect
- once-daily
- ⇒dizziness, decrease appetite, dyspepsia
- carries black box for suicidality
- metabolized by liver and can be mixed with other stimulants
How dose Botulum Toxin work?
- Botulinum toxin works by blocking Ach release from presynaptic terminals (irreversible)
Wht is the surgery for severe, refractory OCD?
Surgery for OCD is anterior capsulotomy/cingulotomy (anterior limb of the internal capsule)
MEdications that INCREASE clozapine levels?
- Clozapine increased by cimetidine, SSRIs, TCAs, VPA, and erythromycin
MEdications that DECREASE clozapine levels?
- Carbemazepine and phenytoin will decrease clozapine levels
________ is a CYP2D6 inhibitor whereas _______ is a CYP2D6 substrate.
- Bupropion is a CYP2D6 inhibitor whereas nortriptyline is a CYP2D6 substrate.
Galantamine is contraindicated in ______ impairment
Galantamine is contraindicated in severe renal and hepatic impairment
Rivastigmine is contraindicated in ________ impairment
- Rivastigmine is contraindicated in hepatic impairment
- Pimavanserin
- inverse agonist at the 5HT-2A receptor
- does not antagonize the D2 receptor like typical antipsychotics.
- only FDA-approved medication for treatment of psychosis in Parkinson’s disease
MOA of Gabapentin
mechanism of action involves inhibition of the alpha 2-delta subunit of voltage-gated calcium channels
Which class of anti-depressants are associated with NARROW-angle glaucoma?
TCAs
antagonist of serotonin 5-HT2A, dopamine (D1, D3, and D4), and alpha receptors (specifically alpha 1 receptors
Clozapine
MOA of lithium-induced nephrogenic diabetes insipidus
- inhibits ADH-stimulated translocation of cytoplasmic urinary aquaporin 2 (AQP2) to the apical membrane on the collecting duct
- down-regulation of channel aquaporin-2 in the luminal wall of the cell’s surface, leading to decreased urine osmolality and increased urine volume (polyuria).
TREATMENT of f lithium-induced nephrogenic diabetes insipidus
- amiloride, a potassium-sparing diuretic that reduces lithium uptake in the cells of the collecting duct improving responsiveness to ADH-stimulated translocation of AQP2 to the membrane of the principal cells.
Buspirone mechanisms of action:
- 5HT1A receptor partial agonist at postsynaptic receptors in the hippocampus and cortex,
- 5HT1A receptor full agonist at presynaptic receptors
- presynaptic dopamine antagonist at D2, D3, and D4 receptors
- partial α1 receptor agonist.
Monitoring in pregnancy on Lithium
- Draw alpha fetoprotein before 20 weeks gestation to rule out neural defects
- High-res fetal US done at 16-18 weeks to rule out cardiac malformations
- At 34 weeks Li levels drawn weekly
How does dutasteride aid in treatment of PMDD?
Medication is a 5 alpha reductase inhibitor that blocks the conversion of progesterone to Allopregnanolone (5α-reduced neurosteroid metabolite) which is indicated in mood symptoms in PMDD
____________ is a metabolite of ________and is less anticholinergic than most other TCAs, making it less sedating, less orthostatic
Nortriptyline is a metabolite of amitriptyline and is less anticholinergic than most other TCAs, making it less sedating, less orthostatic,
Which genetic test should be given before prescribing this psychotropic in Asian pts?
HLA-B*1502 allele; Carbamazepine
- Acetylsalicylic acid, aspirin, can reduce the elimination of valproic acid
- Cholestyramine can reduce the absorption of valproic acid from the intestine.
- Carbamazepine and phenytoin can increase the elimination of valproic acid
- Acetylsalicylic acid, aspirin, can reduce the elimination of valproic acid
- Cholestyramine can reduce the absorption of valproic acid from the intestine.
- Carbamazepine and phenytoin can increase the elimination of valproic acid
Drugs that decrease TCA concentrations
- Drugs that decrease TCA concentrations include ascorbic acid, lithium, barbiturates, and primidone.
- Also cigarette smoking via induction of the cytochrome P450 1A2 enzyme
Interaction of Fluxoitene and Cardic medications?
- Fluoxetine (along with paroxetine) is a strong 2D6 inhibitor ⇒ inhibit the metabolism of commonly used cardiovascular medications (e.g., S-metoprolol).
- Increased levels of S-metoprolol (secondary to 2D6 inhibition of its metabolism) may cause bradycardia such as that experienced by the patient.
- The active metabolite of fluoxetine (norfluoxetine) has a half-life of 2 weeks and thus may cause drug-drug interactions with cardiovascular medications as long as 2-to-3 months after it is discontinued.
*
Z-drugs are metabolized by _______
CYP3A4
Z-drugs are metabolized by _______
CYP3A4
What is indicated in cases of anticholinergic poisoning?
- Physostigmine amplifies the effect of acetylcholine by inhibiting its breakdown. It is indicated in cases of anticholinergic poisoning.
What is given in cases of organophosphate poisoning?
- Pralidoxime works by reactivating acetylcholinesterase. It is given in cases of organophosphate poisoning.
MAO of Zofran
Ondansetron is a 5HT-3 selective serotonin receptor antagonist, and it acts as a centrally acting antiemetic via inhibition of the vagal nerves to the CNS and gastrointestinal tract
Mirtazapine
- Mirtazapine is a ________ antidepressant
- Antagonism ________ → increased firing of NE and 5HT receptors
- Antagonism of _____ and _______ → anxiolytic and hypnotic effects
- _____ receptor blockade→ combat serious GI effects of cancer chemotherapy + appetite stimulation
- Antagonist of ____ receptors → increased somnolence + increased appetite
- ________ blockade → anxiolytic and useful in the treatment of PTSD
- Mirtazapine is a tetracyclic antidepressant
- Antagonism alpha-2 adrenergic → increased firing of NE and 5HT receptors
- Antagonism of 5HT2 and 5HT3 → anxiolytic and hypnotic effects
- 5HT3 receptor blockade→ combat serious GI effects of cancer chemotherapy + appetite stimulation
- Antagonist of H1 receptors → increased somnolence + increased appetite
- Alpha1 adrenergic blockade → anxiolytic and useful in the treatment of PTSD
Tx for TCA toxicity
Sodium Bicarb
TCA toxicity → cardiac arrhythmia, convulsions, confusion, coma, acidosis, and hypotension
only FDA approved for the preventative treatment of major depressive disorder with seasonal pattern
Bupropion
How do you treat ADHD patient with Tourette’s syndrome
- treated with Atomoxetine. Traditional stimulants can worsen tics
What causes Antipsychotic induced priapism?
- due to blockade of the alpha-1 receptor in the corpora cavernosa. Any atypical antipsychotic can cause priapism. Risperidone has the greatest affinity to the alpha 1 adrenergic receptor and thus has the most reports. Olanzapine is the least likely.
_________ Inhibit enzyme that converts ATP to cAMP → suppression of NE release from locus coeruleus
Opioids
Timeframe for alcohol withdrawal
- Alcohol withdrawal tremulousness (the shakes or the jitters) usually begins 6 to 8 hours after cessation of drinking.
- Psychotic and perceptual symptoms begin 8 to 12 hours and
- seizures usually occur between 12 and 24 hours after the last drink.
- The onset of delirium tremens, if it is going to happen, will occur between 72 hours and up to 1 week after the last drink.
Which opioids appear to be weak serotonin reuptake inhibitors and have all been involved in serotonin toxicity
phenylpiperidine series of opioids:
- pethidine (meperidine)
- tramadol
- methadone
- dextromethorphan
- propoxyphene
*
What is Acomplia (rimonabant)
CB-1 receptor blocker that blocks the effects of THC, but side effects of severe depression and SI prevented its entry into the market.
Cocaine______ the concentration of dopamine by _____________ which plays a vital role in reward and mood.
- Cocaine increases the concentration of dopamine by blocking the dopamine reuptake transporters (DAT) which plays a vital role in reward and mood.
What genetics are shown to produce a substantial increase in psychosis with cannabis use.
T_he presence of Val/Val and Val/Met genotypes for_ COMT (Val158Met) in both homozygous and heterozygous genetic compositions → shown to produce a substantial increase in psychosis with cannabis use.
What genetics are shown to produce a substantial increase in psychosis with cannabis use.
- T_he presence of Val/Val and Val/Met genotypes for_ COMT (Val158Met) in both homozygous and heterozygous genetic compositions
- rs2494732 of AKT1 influences
Which active metabolite is responsible for the psychostimulant effect of caffeine?
Paraxanthines
