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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?
Which Parkinson's drug can make L-dopa side effects worse?
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?
Which epilepsy drug can also be used for seizures of eclampsia?
Which epilepsy drug is safe for pregnant women and children?
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?
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?
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?
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?
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
- 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.
The ___ the lipid solubility, the less inhaled anesthetic you need, or the more potent it is.
Which of the inhaled anesthetics has greatest solubility in blood, therefore takes longest to work?
Which inhaled anesthetic has least blood solubility, therefore works fastest?
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?
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?
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.

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