Neuro Pharm Flashcards by Kevin G

Opiod receptors are this type of receptor, and have these classes

G-protein coupled receptors (mu, delta, kappa)

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Receptor that binds morphine and endorphins

Mu opiod receptor

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Receptor that binds enkephalins

Delta opiod receptor

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Receptor that binds dynorphins

Kappa opiod receptor

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Drug category; Clinical Use: cough suppression, diarrhea; SE: respiratory depression, miosis, CNS depression (coma), constipation

Opiod analgesics

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Opiod drug; MOA: full mu agonist; SE: histamine release

Morphine

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Opiod drug; MOA: full mu agonist; other: useful for maintenance, long duration, orally active

Methadone

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Opiod drug; MOA: full mu agonist; SE: muscarinic antagonist (doesn’t cause miosis), don’t combine with SSRIs or MAOIs

Meperidine

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Opiod drug; MOA: full mu agonist (the other commonly used opiod drug besides morphine)

Fentanyl

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Opiod drug; MOA: partial mu agonist; given in combination with NSAIDS, antitussive

Codeine

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Dextramethorphan (antitussive), diphenoxylate (antidiarrheal), loperamide (antidiarrheal)

OTC opiod analgesics

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Opiod antagonist; short half-life; IV; used for acute opiod overdose

Naloxone

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Opiod antagonist; PO; used to reduce ethanol craving (given to alcoholics)

Naltrexone

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Anxiety, GI distress, gooseflesh, muscle spasms, rhinorrhea, sweating

Abstinence syndrome (withdrawal from opiods)

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Phenytoin, carbamazepine, topiramate, lamotrigine, valproic acid

Epilepsy drugs that block Na channels

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epilepsy drug; MOA: blocks Na channels; SE: gingival hyperplasia, hirsutism, hydantoin fetus, megaloblastic anemia (decreases folate absorption)

Phenytoin

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epilepsy drug; MOA: blocks Na channels; SE: blood dyscrasias, teratogen

Carbamazepine

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epilepsy drug; MOA: blocks Na channels; SE: Steven-Johnson syndrome

Lamotrigine

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epilepsy drug; MOA: blocks Na channels, (inc GABA); SE: kidney stones

Topiramate

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epilepsy drug; MOA: blocks Na channels, (inc) GABA, (-) T-type Ca++ channels; SE: rare fatal hepatotoxicity, causes fetal NTDs

Valproic acid

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Ethosuximide, Valproic acid

Epilepsy drugs that block thalamic T-type Ca++ channels

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Topiramate, Valproic acid, Benzodiazepines, phenobarbitol, gabapentin

Epilepsy drugs that increase GABA

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epilepsy drug; MOA: (inc) GABA; SE: dependence (first line for acute seizures)

Benzodiazepines (diazepam, lorazepam)

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epilepsy drug; MOA: (inc) GABA; SE: dependence (first line for pregnant women, children)

Phenobarbitol (barbiturate)

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epilepsy drug; MOA:(-) T-type Ca++ channels; SE: fatigue, GI, headache, Steven-Johnson Syndrome

Ethosuximide

epilepsy drug; MOA: (inc) GABA; SE: sedation, ataxia

Gabapentin

Which acts faster, highly blood soluble anesthetics or low blood soluble anesthetics?

Low solubility in blood = Rapid inducation and recovery.

What effect does lipid solubility have on anesthetics.

High lipid solubility = high potency

What effect does minimal alveolar concentration of anesthetics have on their potency?

As MAC increases potency decreases.

List the inhaled anesthetics

Halothane, -flurane, NO2

What inhaled anesthetic has hepatotoxicity?

Halothane

What inahled anesthetic has nephrotoxicity

Methoxyflurane

What inhaled anesthetic is a proconvulsant?

Enflurane

Increase the duration of Cl- channel opening, thereby facilitating GABAa action (decreases neuron firing)

Barbiturates

Increase the frequency of Cl- channel opening, thereby facilitating GABAa action (decreases neuron firing)

Benzodiazepines

zepams, zolams, and chlordiazepoxide

Benzodiazepines

Drug used to treat benzodiazepine overdose, competitive antagonist at GABA receptor

flumazenil

(TOM thumb) triazolam, oxazepam, midazolam

Short-acting benzodiazepines

B.B. King on OPIATES PROPOses FOOLishly (Barbiturates, benzodiazepines, Ketamine, opiates, propofol)

Intravenous anesthetics

High potency barbiturate used for induction of anesthesia in short procedures, decreases cerebral blood flow (IV anesthetic)

Thiopental

Benzodiazepine that is the most common drug used for endoscopy, may cause severe postoperative respiratory depression (IV anesthetic)

Midazolam

A PCP analog used as a dissociative anasthetic, decreases cerebral blood flow (IV anesthetic)

Ketamine (arylcyclohexamines)

2 opiates used with other CNS depressants during general anesthesia (IV anesthetics)

Morphine, fentanyl

Used for rapid induction of anesthesia and short procedures, less postoperative nausea than other drugs (IV anesthetic)

Propofol

What are the Local anesthetics?

Esters - end in caine, Amide end in -caine but have a second I

Local anesthetics MOA

Bloack Na channels (preferentially bind activated Na channels)

What fibers are affected first by loacal anesthetics?

Small, myelinated fibers. Pain first, Pressure is last.

What do you coadminister with local anesthetics and why?

Vasoconstrictors to enhance local action (except cocaine!)

What local anesthetics causes CNS excitation and severe cardiovascular toxicity?

Bupivicaine

What are neuromuscular blocking drugs used for?

Muscle paralysisin surgery or mechanical ventilation.

What receptor do NMJ blocking drugs target?

What is the only depolarizine NMJ blocking drug and what are it's two phases?

Succinylcholine. Phase 1 = prolonged depolarization. Phase 2 = Repolarized but bloacked.

Effect of giving cholinesterase inhibitors in each phase of succinylcholine action.

Phase 1: Cholinesterase inhiitors makes it worse. Phase 2: Reversed by cholinesterase inhibitors

What are the nondepolarizing NMJ blockers?

Have cur in the name (end in cararine, curium or curonium)

How do you reverse a nondepolarizing NMJ block?

AChE inhibitors (neostigmine, edrophonium)

How do you treat malignant hyperthermia or neuroleptic malignant syndrome?

Dantrolene (prevents release of Ca2+ from SR)

What causes malignant hyperthermia?

Using inhaled anesthetics (except NO2) + succinylcholine)

What is the mneumonic for Parkinson's treatments

BALSA (Bromocriptine, Amantadine, Levodopa, Selegiline, Antimuscarinics)

What are the 4 treatment classes for Parkinson's?

Agonize dopamine receptors (bromocriptine), Inc Dopamine (Amantadine, Ldopa/carbidopa) Prevent dopamine breakdown (MAO B inh, selegiline), Curb excess cholinergics (benztropine, no effect on bradykinesia)

What is the treatment for essential or familial tremors?

Beta blockers

How does the L-dopa/carbidopa treatment work?

L-dopa crosses the blood brain barrier and is converted in CNS to dopamine. Carbidopa inhibits peripheral decarboxylase.

What parkinson drug causes arrhythmais?

L-dopa (when it's converted to dopamine in periphery)

What drug is coadministered with L-dopa in parkinson's but may enhance its side effects?

Selegiline (MAO-B inhibitor)

Treatment of migraines

Sumatripan. 5-HT 1D agonist. Causes vasoconstriction. Short half-life. (side effect = coronary vasospasm)

Contraindications for sumatripan

CAD or prinzmetals (causes coronary vasospasm)

Memantine - mOA?

NMDA receptor antagonist - helps prevent excitotoxicity (mediated by Ca2+)

Memantine - AEs?

Dizziness, confusion, hallucinations

Donepezil - MOA?

Acetylcholinesterase inhibitor

Donepezil - AEs?

Nausea, dizziness, insomnia

Tetrabenazine - MOA?

inhibits VMAT | - limits dopamine vesicle packaging & release

Reserpine - MOA?

inhibits VMAT | - limits dopamine vesicle packaging & release

Haloperidol - MOA?

Dopamine receptor antagonist

Huntington's drugs?

Tetrabenazine, Reserpine, & Haloperidol

Sumatriptan - MOA?

5-HT(1B/1D)-agonist - inhibits Trigeminal nerve activation - prevents vasoactive peptide release - induces vasoconstriction - ½-life < 2 hours

Dantrolene - clinical uses?

- Malignant hyperthermia (rare, life-threatening side-effect of inhalation anesthetics -- except NO2 -- & succinylcholine) - Neuroleptic malignant syndrome (toxicity of antipsychotics)