Neuro and Psych Pharm
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- Parkinson's drugs that agonize dopamine receptors =
- bromocriptine, pramipexole, ropinirole
- Parkinson's drugs that increase dopamine availability to CNS =
- amantadine, L-dopa/carbidopa
- Parkinson's drugs that prevent dopamine breakdown =
- selegiline (MAO-B inhibitor), entacapone, tolcapone (COMT inhibitors)
- Parkinson's drug that curbs excess cholinergic activity =
- benztropine (antimuscarinic)
- Which Parkinson's drug, over long term use, can cause dyskinesia following dosage and akinesia between doses?
- L-dopa/carbidopa
- Which Parkinson's drug can make L-dopa side effects worse?
- Selegeline
- What do you give for cluster HA and acute migraine?
- Sumatriptan - 5HT 1D agonist, causes vasoconstriction {tox: coronary vasospasm and mild tingling}
- Which 3 epilepsy drugs are contraindicated in pregnant women?
-
- phenytoin (teratogen)
- carbamazepine (teratogen)
- valproic acid (spina bifida)
*All 1st line for tonic-clonic - Which epilepsy drugs can cause Stevens-Johnson syndrome?
-
- ethosuximide
- lamotrigine - Which epilepsy drug can also be used for night terrors and sleep walking because it shortens Stage 4 of the sleep cycle?
- Benzodiazepines
- Which epilepsy drug can also be used for seizures of eclampsia?
- Benzodiazepines
- Which epilepsy drug is safe for pregnant women and children?
- Phenobarbital
- How do you Tx a benzodiazepine overdose?
- Flumazenil - competitive GABA receptor antagonist!
- What are first-line for tonic-clonic generalized seizures? (3)
-
- phenytoin
- carbamazepine
- valproic acid - What is first-line for absence seizures?
-
- ethosuximide
- valproic acid also used - What are 2 drugs for status epilepticus, a medical emergency?
-
- phenytoin (prophylaxis)
- benzodiazepines (acute) - Which epilepsy drug is used to help alcohol withdrawal?
- Benzodiazepines
- Which epilepsy drug is least sedating and also appropriate for myoclonic seizures?
- Valproic acid
- Name 4 neuroleptic drugs commonly used for schizophrenia:
-
- thioridazine
- haloperidol
- fluphenazine
- chlopromazine - How do the neuroleptics work?
- block D2 receptors (schizophrenia is too much dopamine)
- What is the evolution of side effects with long-term neuroleptics use?
-
4 hrs - acute dystonia
4 day - akinesia
4 wks - akathisia
4 mon - tardive dyskinesia - What is Neuroleptic Malignant syndrome?
-
- muscle rigidity
- hyperpyrexia
- myoglobinuria
- autonomic dysfunction - What are the bad side effects of neuroleptics? (6)
-
- prolactinemia, gynecomastia
- hypotension (alpha blocker)
- sedation (antihistamine)
- dry mouth (anticholinergic)
- EPS side effects
- neuroleptic maligant synd. - What are the atypical anti-psychotics? (3)
-
- olanzapine
- clozapine
- risperidone - How do atypical antipsychotics work?
- block 5HT 2 and dopamine receptors - less EPS and anticholinergic toxicities than other antipsychotics
- What else can Olanzapine be used for, besides schizophrenia?
- OCD, anxiety, depression, mania, Tourette's
- What is a specific side effect of Clozapine?
- agranulocytosis - check WBCs every week
- What do you give for bipolar mood stabilization?
- Lithium
- What are side effects of Lithium?
-
- tremor
- polyuria (ADH antagonist)
- hypothyroidism
- teratogen!! - What are the names of 4 SSRI's?
-
- fluoxetine
- sertraline
- paroxetine
- citalopram - What are 3 side effects of SSRI's?
-
- GI distress
- sexual dysfunction
- if used in combo with MAOI, serotonin syndrome - What are the manifestations of Serotonin Syndrome?
-
- hyperthermia
- muscle rigidity
- cardiovascular collapse - How long does it take antidepressants to work?
- 2-3 wks
- Name some TCA's: (6)
-
- amitriptyline
- nortriptyline
- imipramine
- desipramine
- clomipramine
- doxepin - What do TCA's block?
- reuptake of NE and 5HT
- What can Imipramine also be used for besides major depression?
- bedwetting (dec. Stage 4 sleep)
- What can Clomipramine also be used for besides major depression?
- OCD
- What are 3 toxicities of TCAs?
-
- convulsion
- coma
- cardiotoxicity (arrhythmia) - Amitriptyline has worse ____ effects than Nortriptyline.
- anticholinergic! (recall QBank question where Amitriptyline exacerbated ACUTE ANGLE GLAUCOMA because it contracted pupillary constrictor to dilate pupil)
- Which TCA is least sedating?
- Desipramine
- Name 5 heterocyclic antidepressants:
-
- bupropion
- venlafaxine
- mirtazapine
- maprotiline
- trazodone - What else is Bupropion used for other than major depression?
- smoking cessation
- What are toxicities of Bupropion?
-
- stimulant
- HA
- seizures in bulimics
*NO sexual side effects - What else is Venlafaxine used for besides major depression?
- GAD - inhibits NE/5HT/DA reuptake
- What are toxicities of Venlafaxine?
-
- elevate BP
- nausea
- sedation
- constipation - What does Mirtazapine block?
-
1) a2 antagonist - inc. release of more NE and 5HT
2) block 5HT 2 & 3 receptors - What are toxicities of Mirtazapine? (4)
-
- inc. appetite
- wt. gain
- dry mouth
- sedation - What does Maprotiline block?
- NE reuptake
- What are 2 toxicities of Maprotiline?
-
- sedation
- orthostatic hypotension - What does Trazodone inhibit?
- 5HT reuptake
- What are side effects of Trazodone? (4)
-
- sedation
- nausea
- PRIAPISM
- orthostatic hypotension - What are 2 MAOI's?
-
- phenelzine
- tranylcypromine - What are 4 things you should NOT ingest when taking a MAOI?
-
- tyramine foods (cheese, wine, beer)
- SSRI (serotonin syndrome)
- beta agonist (serotonin syndrome)
- meperidine (a narcotic) - Name 6 inhaled anesthetics:
-
- halothane
- enflurane
- isoflurane
- sevoflurane
- methoxyflurane
- nitrous oxide (N2O) - The ___ the solubility in blood, the faster the inhaled anesthetic works.
- lower
- The ___ the lipid solubility, the less inhaled anesthetic you need, or the more potent it is.
- higher
- Which of the inhaled anesthetics has greatest solubility in blood, therefore takes longest to work?
- Halothane
- Which inhaled anesthetic has least blood solubility, therefore works fastest?
- N2O
- What are effects of inhaled anesthetics?
-
- myocardial depression
- respiratory depression
- nausea/emesis
- inc. cerebral blood flow - What are specific toxities of halothane, methoxyflurane, enflurane?
-
Halothane - hepatotoxicity
Methoxyflurane - nephro
Enflurane - seizure - What is a rare but dangerous toxicity of inhaled anesthetics?
- Malignant hyperthermia!
- Which barbiturate is used IV to induce anesthesia and short surgical procedures?
- Thiopental - high potency, high lipid solubility, rapid entry into brain
- Which benzodiazepine is used as IV anesthetic for endoscopy?
- Midazolam - reverse effects with Flumazenil!
- Which IV anesthetic is a PCP analog?
- Ketamine - cardiovascular stimulant, cause bad stuff like hallucination, nightmares, disorientation
- Which 2 opiates are commonly used with other CNS depressants during general anesthesia?
-
- morphine
- fentanyl - Which short-acting, rapid-inducing IV anesthetic has less postoperative nausea than Thiopental?
- Propofol
- What are the ester local anesthetics? (3)
-
- cocaine
- procaine
- tetracaine - What are the amide local anesthetics? (3)
-
- lidocaine
- bupivacaine
- mepivacaine - How do local anesthetics work?
- block Na channels by binding to inside of channel (amides enter membrane as uncharged form, but bind as charged form)
- If you want to locally anesthetize infected tissue, what is the rule?
- Give bigger dose. Infected tissue is acidic so drug will be protonated/charged and not easily enter membrane.
- Which nerve fiber will be blocked first: small unmyelinated pain fibers or small myelinated autonomic fibers?
- Small unmyelinated pain fibers - size more important than myelination
- When receiving a local anesthetic, what is the order in which you lose sensations?
-
1) pain
2) temperature
3) touch
4) pressure - How do you enhance the action of a local anesthetic?
- Give epinephrine to vasoconstrict.
- When would you use local anesthetics?
-
- minor procedures
- spinal anesthesia - Which local anesthetic has severe cardiovascular toxicity?
- Bupivacaine (amide)
- Which local anesthetic can cause arrhythmia?
- Cocaine
- What happens if someone is allergic to cocaine/procaine/tetracaine?
- Give an amide instead.
- How does Succinylcholine work?
- Depolarizing neuromuscular blocker. Binds selectively to motor nicotinic receptor on muscle cell.
- What is Phase 1 of succinylcholine action?
- Prolonged depolarization for which there is no antidote. Depolarization action potentiated if use cholinesterase inhibitors.
- What is Phase 2 of succinylcholine action?
- Repolarized muscle cell but still blocked. Here can use cholinesterase inhibitors to raise ACh concentration and overcome succinylcholine.
- What are the non-depolarizing neuromuscular blockers?
-
- tubocurarine
- atracurium, mivacurium
- pancuronium, vecuronium, rapacuronium - How does Vecuronium work? What can block it?
- Compete with ACh for receptors on muscle. Reverse effect with cholinesterase inhibitors.
- What do you give for malignant hyperthermia and neuroleptic malignant syndrome? What is its mechanism?
- Dantrolene - my favorite. Blocks release of Ca from SR of skeletal muscle so muscle can't contract and cause hyperthermia.