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21 Cards in this Set

  • Front
  • Back
Baclofen
GABAb agonist, causes hyperpolarization and inhibits release of excitatory transmitters

oral, 3hλ, maybe best intrathecal to reduce peripheral sx

there is more
Tizanidine
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
Cyclobenzaprine
sedative in brainstem

anticholinergic activity

temporary releaf of actue msucle spasms

may produce confusion and transient visual hallucinations
carisoprodol
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.
Dantrolene
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
Botox
prevents release of ACh from presynaptic nerve terminals

IM or intradermal for dystonia or sweatiness
Methylphenidate
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
Ritalin
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
Amphetamine
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
Atomoxetine
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
Caffeine
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
Phenytoin
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
Carbamazepine
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
Phenobarbital
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
Gabapentin
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
Ethosuximide
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
Valproic Acid
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
Diazepam vs. Seizures
DOC for status epilepticus, given IV

Pregnancy Category D
DOC for partial seizures
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
DOC for absence seizures
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
DOC vs combined absence + tonic clonic if they occur together
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