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21 Cards in this Set
- Front
- Back
Baclofen
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GABAb agonist, causes hyperpolarization and inhibits release of excitatory transmitters
oral, 3hλ, maybe best intrathecal to reduce peripheral sx there is more |
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Tizanidine
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clonidine analogue, alpha 2 agonist
reinforces pre-and post-synaptic inhibition in the psinal cord, inhibits pain transmission used to reduce chornic muscle spasticity causes significant sedation |
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Cyclobenzaprine
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sedative in brainstem
anticholinergic activity temporary releaf of actue msucle spasms may produce confusion and transient visual hallucinations |
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carisoprodol
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may interrupt neural communcationwithin CNS reticular formation and spinal cord
sedation, altered pain perception induces CYP's metabolized rapidly to meprobamate, acts like barbituate; a popular drug of abuse. |
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Dantrolene
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interferes with release of Ca2+ in SR
rapidly contracting muscles more sensitive than slowly contracting, heart okay used for malignant hyperthermia and neuroleptic malignant syndrome |
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Botox
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prevents release of ACh from presynaptic nerve terminals
IM or intradermal for dystonia or sweatiness |
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Methylphenidate
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Ritalin: an amphetamine like drug, esp DA CNS neurons
Short λ morning, lunchtime Uses: Narcolepsy, ADHD Effects: euphoria, alertness, increased energy, anorexia, increased BP decreased HR Side Efx: anxiety, insomnia, irritability at High [Rx]: psychosis, stereotypic fixations, increased HR & BP Withdrawal: paranoia, hunger, increased need for sleep, severe depression, suicidal behavior |
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Ritalin
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Methylphenidate: an amphetamine like drug, esp DA CNS neurons
Short λ morning, lunchtime Uses: Narcolepsy, ADHD Effects: euphoria, alertness, increased energy, anorexia, increased BP decreased HR Side Efx: anxiety, insomnia, irritability at High [Rx]: psychosis, stereotypic fixations, increased HR & BP Withdrawal: paranoia, hunger, increased need for sleep, severe depression, suicidal behavior |
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Amphetamine
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Aderall: used for ADHD if Methylphenidate (Ritalin) is ineffective, once used for weightloss with poor efficacy and many side effex
Effects: euphoria, alertness, increased energy, anorexia, increased BP decreased HR Side Efx: anxiety, insomnia, irritability at High [Rx]: psychosis, stereotypic fixations, increased HR & BP Withdrawal: paranoia, hunger, increased need for sleep, severe depression, suicidal behavior |
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Atomoxetine
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Selective Norepinephrine Reuptake Inhibitor used for ADHD
no abuse potential CV effects of beta agonists: increased HR & BP, should not be used iwth vasopressors (DA, epi, midodrine, NE, phenylephrine) contraindicaed with MAOI's GI & Dizziness |
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Caffeine
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Blocks adenosine receptors in CNS (adenosine = sedation, blood vessel dilation, broncospasm, decreased NT relase)
increases cAMP by inhibiting phosphodiesterase increases mental alertness, simulates heart, dilates coronary arteries, constricts cerebral blood vessels, bronchodilation, increased gastric acid, diuresis (both increased renal blood flow and deacreased ADH) 5+ cups/day: anxiety, insomnia, tachycardia, hypertension, psychosisi withdrawal: HA, fatigue, bad mood |
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Phenytoin
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Blocks sustained high frequency repetitive firing of neurons by prolonging inactivation of the NA+ channel
effective against partial seizures and generalized tonic clonic NOT vs. absence not water soluble (not injected), 90% plasma bound, binds thyroid binding globulin, will mess with thyroid fnx tests. displaced by pheylbutazone or sulonamides elimination is zero order at theraputic [Rx], λ 12-36 hours, theraputic range is small; induces CYP's, increases oral contraceptive breakdown, warfarin conentration will increase dramatically with phenytoin; carbamazepine increases metabolism of phenytoin. Toxicity: ginigval hyperplasia and hirsutism, CNS (there are many others) Known Teratogen, category D |
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Carbamazepine
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DOC for partial seizures: blocks sustained high frequency repetitive firing of neurons by prolonging inactivation of the NA+ channel, also used for tonic-clonic, bipolar, and trigeminal neuralgia
Best after meal, induces CYP3A (phenytoin, primidone, ethosuximide, valproic acid clonazepam, haloperidol & oral contraceptives), λ drops 36 to 24h w/ use Cimetidine, fluoxeitine, isoniazid & erythromyin inhibit carbamazepine matabolism SdEfx: GI, CNS issues + Ideosyncratic blood dyscrasias like aplastic anemia, or agranulocytosis at high [Rx] Skin rash = hypersensitivity Stephens Johnson Syndrome in HLAB1502 (pan-Asia) Pregnancy Category D: evidence of serious birth defects |
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Phenobarbital
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prolongs opening of chloride channel at GABAa
used for partial and generalized tonic-clonic seizures CNS depressant Primidone is metabolized to phenobarbital Pregnancy Cateogry D: do not use |
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Gabapentin
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GABA analog unknown mechanism of action, not direct agonist
adjunct treatmetn for partial seizures and generalized tonic-clonic seizures, also for neuropathic pain, bipolar, anxiolytic Kidney, 6h λ SdEfx: generally resolve in weeks on drug (Dizziness, drowsinesss, ataxia, HA, tremor, weight gain) Pregnancy Category C |
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Ethosuximide
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First choice drug for absence seizures
T-type pacemaker Ca2+ channels in thalamus, ethosuximide reduces low-threshold Ca2+ current well absorbed, 2x/day to avoid GI effects valproic acid decreases clearance gastric pain, decreased by gradually increasing dose preganncy cateogry C: unknown effects |
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Valproic Acid
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Blocks high-frequency reptitive firing probably of Na_
DOC vs combined absence + tonic clonic if they occur together Also used for myoclonic seizures, bipolar, migraine prophylaxis well absorbed, given after meals to decrease toxicity 9-19hλ inhibits its own metabolism, as well as that of phenytoin & carbamazepine Toxicity: Idiosyncratic sever hepatotoxicity, pregnancy cateogry D; weight gain, fine tremor, sedation w/ phenobabital |
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Diazepam vs. Seizures
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DOC for status epilepticus, given IV
Pregnancy Category D |
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DOC for partial seizures
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Carbamazepine: blocks sustained high frequency repetitive firing of neurons by prolonging inactivation of the NA+ channel, also used for tonic-clonic, bipolar, and trigeminal neuralgia
Best after meal, induces CYP3A (phenytoin, primidone, ethosuximide, valproic acid clonazepam, haloperidol & oral contraceptives), λ drops 36 to 24h w/ use Cimetidine, fluoxeitine, isoniazid & erythromyin inhibit carbamazepine matabolism SdEfx: GI, CNS issues + Ideosyncratic blood dyscrasias like aplastic anemia, or agranulocytosis at high [Rx] Skin rash = hypersensitivity Stephens Johnson Syndrome in HLAB1502 (pan-Asia) Pregnancy Category D: evidence of serious birth defects |
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DOC for absence seizures
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Ethosuximide
T-type pacemaker Ca2+ channels in thalamus, ethosuximide reduces low-threshold Ca2+ current well absorbed, 2x/day to avoid GI effects valproic acid decreases clearance gastric pain, decreased by gradually increasing dose preganncy cateogry C: unknown effects |
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DOC vs combined absence + tonic clonic if they occur together
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Valproic Acid
Blocks high-frequency reptitive firing probably of Na_ Also used for myoclonic seizures, bipolar, migraine prophylaxis well absorbed, given after meals to decrease toxicity 9-19hλ inhibits its own metabolism, as well as that of phenytoin & carbamazepine Toxicity: Idiosyncratic sever hepatotoxicity, pregnancy cateogry D; weight gain, fine tremor, sedation w/ phenobabital |