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42 Cards in this Set
- Front
- Back
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Phenytoin
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Anti-seizure
-1st line for tonic-clonic and status epilepticus (prophylaxis) -mech: use-dependant blockade of Na channels causing increased refractory period, inhibition of glutamate release from excitatory presynaptic neurons. -ae - nystagmus, ataxia, SLE-like syndrome, induction of CYP450, gingival hyperplasia in kids, peripheral neuropathy, hirtuism, megaloblastic anemia, terato - fetal hydantoin syndrome |
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Phenobarbitol
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Anti-seizure
-can be used for all partial seizures and tonic-clonic -mech: facilitates GABAa action by increasing duration of Cl channel opening, thus decreasing neuron firing -sedation, tolerance, dependence, induction of CYP450 |
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Uses for barbiturates, mech, AE
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sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopentol)
-mech: facilitate GABAa action by increasing DURATION of Cl channel opening, thus decreasing neuron firing -ae: dependence, additive CNS depression with alcohol, drug interactions with CYP450 |
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Carbamazepine
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Anti-seizure
-1st line for tonic-clonic seizures -mech: blocks Na channels -ae: diplopia, ataxia, agranulocytosis, aplastic anemia, liver tox, teratogenesis, induction of P450, SIADH, Steven-Johnson syndrome |
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Lamotrigine
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Anti-seizure
-used for partial and tonic-clonic seizures -mech: blocks voltage gated Na channels -ae: Steven-Johnsons syndrome (mailaise and fever followed by rapid onset of erythematous purpuric macules (oral, ocular, genital) with skin lesions progressing to epidermal necrosis and sloughing) |
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Gabapentin
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Anti-seizure
-for partial and tonic-clonic seizures -also used for peripheral neuropathy, bipolar disorder -mech: inhibits Ca channels ae: sedation, ataxia |
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Topiramate
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Anti-seizure
-partial and tonic-clonic seizures -mech: blocks Na channels, increases GABA action -ae: sedation, mental dulling, kidney stones, weight loss |
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Valproic acid
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Anti-seizures
-1st line for tonic-clonic seizures, also used for absence and myoclonic seizures -mech: blocks Na channels, increases GABA concentration -ae: neural tube defects in fetus (inhibits folic acid absorption), tremor, weight gain |
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Ethosuximide
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Anti-seizure
-1st line for absence seizures (only thing it treats) -mech: blocks thalamic T-type Ca channels -ae: GI upset, fatigue, headache, urticaria, Steven-johnson syndrome |
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Tiagabine
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Anti-seizure
-only treats partial seizures -mech: prevents GABA uptake |
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Vigabatrin
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Anti-seizure
-only treats partial seizures -mech: irreversibly inhibits GABA transaminase, increasing GABA concentration |
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Benzodiazapines (diazepam or lorazepam)
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Anti-seizure, anxiety, spasicity, detox
-only treats acute status epilepticus -mech: increases GABAa action by increasing the FREQUENCY of Cl channel opening -ae: decreases REM sleep, dependance, additive CNS depression (less than barbiturates) tx overdose with flumazenil (competitive antagonist at GABA benzo receptor) |
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Non benzo hypnotics
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Zolpedem, zaleplon, eszopiclone
-mech: act at benzo receptor -use: insomnia -ae: ataxia, headaches, confusion, short duration bc of rapid metabolism by liver enzymes. low risk of dependance |
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Inhaled anesthetics
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halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, NO
-mechanism unknown -effects - myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand) -ae: hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane), malignant hyperthermia |
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IV anesthetics
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(BB King on OPIATES PROPOses FOOLishly)
-Barbiturates - thiopental - high potency, high lipid solubility. Used for induction of anesthesia and short surgical procedures -Benzodiazepines - midazolam used for endoscopy, may cause severe postoperative respiratory depression, decrease in BP, and amnesia -Ketamine - PCP analog that acts as a dissociative anesthetic. Blocks NDMA (glutamate) receptors. Cardiovascular stimulant, causes disorientation, hallucination, bad dreams, increases cerebral blood flow -opiates - morphine, fentanyl used for general anesthesia -propofol: used for rapid induction and short procedures, less nausea than thiopental. potentiates GABAa |
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Local anesthetics
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amides all have ii in name: lidocaine, mepivacaine, bupivacaine. esters - procaine, cocaine, tetracaine
-mech: block Na channels by binding to specific receptors on inner portion of channel, preferentially to activated Na channels, so most effective in rapidly firing neurons. -ae: CNS toxicity, cardiovascular tox (bupivicaine), htn, hypotension, arrhythmias (cocaine) |
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Depolarizing neuromuscular blocking drug
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Succinylcholine
-mech: competitive agonist of the postsynaptic nicotinic receptor, binds so strongly to the receptor that prolonged depolarization occurs, initially causing generalized skeletal muscle contraction that is short-lived, flaccid paralysis follows -ae: hypercalcemia and hyperkalemia - selective for motor nicotinic receptor |
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Nondepolarizing neuromuscular blocking drugs
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Tubocurarine, atracurium, mivacurion, pancuronium, vecuronium, rocuronium
-mech: competitively antagonize binding of ACh to the postsynaptic nicotinic receptor, causing skeletal muscle paralysis. Can be used in intubation |
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Dantrolene
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used to tx malignant hyperthermia (caused by inhaled anesthetics) and neuroleptic malignant syndrome (caused by antipsychotics)
-mech: prevents release of Ca from the sarcoplasmic reticulum of skeletal muscle by blocking Ca-ATPase, which normally maintains a low cytoplasmic concentration of calcium |
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Bromocriptine
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Parkisons
-agonizes dopamine receptors |
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Amantadine for Parkinsons
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-increases dopamine
-ae: ataxia |
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L-dopa
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converted to dopamine in CNS
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Selegiline
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Parkinsons
selective MAO type B inhibitor prevents dopamine breakdown |
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Entacapone, tolcapone
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Parkinsons
COMT inhibitors prevent L-dopa degradation in the periphery |
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Benztropine
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Parkinsons (Park your mercedes BENZ)
-antimuscarinic improves tremor and rigidity but has no effect on bradykinesia |
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Mnemonic for Parkinsons drugs
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BALSA
-bromocriptine -amantadine -levodopa (with carbidopa) -selegiline (and COMT inhibitors) -Antimuscarinics |
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Carbidopa
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peripheral decarboxylase inhibitor, given with L-dopa to increase bioavailability to the brain and limit peripheral side effects
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Memantine
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Alzheimers
-mech: NDMA antagonist, helps prevent exitotoxicity (mediated by Ca) -ae: dizziness, confusion, hallucinatioin |
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Donepezil
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Alzheimers
-mech: acetylcholinesterase inhibitor -ae: nausea, dizziness, insomnia |
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Reserpine
tatrabenazine |
Huntingtons
amine depleting |
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Haloperidol for Huntingtons
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dopamine receptor antagonist
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Sumatriptan
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Acute migrane, cluster headaches
-mech: 5-HT agonist, causes vasoconstriction, inhibition of trigeminal activation, and vasoactive peptide release ae: coronary vasospasm |
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Bethanechol
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Cholinomimetic
activates bowel and bladder smooth muscle -tx: postoperative and neurogenic ileus and urinary retention |
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Carbachol
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cholinomimetic
-tx: glaucoma pupillary contraction |
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Pilocarpine
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Cholinomimetic
-mech: potent stimulator of sweat, tears, saliva. contracts ciliary muscle of eye, pupillary sphincter |
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Methacholine
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Cholinomimetic
-mech: stimulates muscarinic receptors in airways -tx: test for diagnosis of asthma |
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Neostigmine
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Anticholinesterase (indirect cholinomimetic)
-mech: increases endogenous ACh, no CNS penetration -tx: postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postop) |
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Pyridostigmine
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Anticholinesterase (indirect cholinomimetic)
-tx: myasthenia gravis, doesn't penetrate CNS |
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Edrophonium
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Anticholinesterase (indirect cholinomimetic)
-tx: diagnosis of myasthenia gravis |
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Physostigmine
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Anticholinesterase (indirect cholinomimetic)
--tx: glaucoma (crosses BBB, CNS side effects and atropine overdose) |
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Echotriophate
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Anticholinesterase (indirect cholinomimetic)
-tx: glaucoma |
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Hexamethonium
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Nicotinic antagonist
-tx: ganglionic blocker, prevents vagal reflexes (ex bradycardia) -ae: orthostatic hypotension, blurred vision, constipation, sexual dysfunction |
