Lee Flashcards
Diazepam
- MOA: GABAa agonist*** -> hyper polarize (open Cl- channels)
- indications: chronic spasm due to cerebral palsy, stroke, spinal cord injury or acute spams due to muscle injury***
Baclofen
- MOA: GABAb agonist -> hyper polarize (inhibit Ca2+ influx, increase K+ efflux)
- category C pregnancy drug
Tizanidine
- MOA: alpha2-adrenergic agonist in SPINAL CORD***
- do NOT use w/ CYP1A2 inhibitors (fluvoxamine and ciprofloxamine)**
- AE: CYP1A2 inhibition and inducution***
Cyclobenzaprine
- MOA: inhibits stretch reflex in spinal cord
- do NOT use w/ MAO -> seizures* or ptxs w/ past MI, arrhythmias, heart block, conduction probs, or CHF*
Dantrolene
- MOA: block RYR1 channels in SR of skeletal muscle
- indications: MALIGNANT HYPERTHERMIA***
- AE: HEPATOTOXIC and severe DIARRHEA
Botulinum Toxin
-MOA: inhibits synaptic exocytosis of vesicles by cleaving SNAP-25 or synaptobrevin-2 -> flaccid paralysis
Levodopa aka L-DOPA
- MOA: precursor to DA -> metabolized to DA by DOPA decarboxylase
- AE: ANOREXIA, NAUSEA, TACHYCARDIA, postural HYPOTENSION, PSYCHIATRIC PROBS
Bromocriptine
-MOA: 1st gen Ergot D2 agonist
Pramipexole
- MOA: 2nd gen Non-ergot D3 agonist
- monotherapy for mild Parkinson’s
Amantadine
- MOA: increase DA synthesis and release and decrease reuptake
- can cause urinary retention and peripheral edema
Selegiline
- MOA: selective irreversible inhibitor of MAO-B
- transdermal to prevent amphetamine metabolites
- do NOT use w/ MEPERIDINE (opioid)**
- AE: drug interactions w/ MEPERIDINE***
Rasagiline
- MOA: selective irreversible inhibitor of MAO-B
- no metabolites
Tolcapone
- MOA: selective reversible inhibitor of COMT
- PERIPHERAL and CENTRAL effects
- NOT used in liver disease/damage
- AE: hepatic failure
Entacopone
- MOA: selective reversible inhibitor of COMT
- only PERIPHERAL effects
Benztropine
- MOA: anticholinergic and antimuscarinic
- do NOT use in children <3 y/o*
- AE: blurred vision, confusion, mydriasis, constipation, urinary retention*
Trihexphenidyl
- MOA: anticholinergic and antimuscarinic
- do NOT use w/ NARROW ANGLE GLAUCOMA**
- AE: same + glaucoma and muscle weakness
what drug are you not suppose to use w/ drugs like nefazodone, boceprevir, delavirdine or other non-nucleoside reverse transcriptase inhibitors that are a substrate of CYP3A4?
carbamazepine
-induces CYP3A4**
oxcarbazepine
-does not produce the metabolite causing CYP interactions like carbamazepine does
Phenytoin***
- MOA: binds to Na+ channel in inactive state
- used for STATUS EPILEPTICUS*** (injection)
- AE: DIPLOPIA, ATAXIA, GINGIVAL HYPERPLASIA, HIRSUTISM***
Topiramate***
- MOA: binds voltage-gated Na+ channels, GABAa receptor subtypes, and AMPA or kainate receptors
- NOT used w/ alcohol or ptxs w/ METABOLIC ACIDOSIS who take meformin***
- AE: IMPAIRED EXPRESSIVE LANGUAGE***** and decreased serum bicarb
Valproic acid***
- MOA: blocks Na+ channels; increases GABA to brain neurons and enhances GABA action
- not used in HEPATIC DISEASE (HEPATOTOXIC)***
- TERATOGEN -> not used in women of childbearing age -> NEURAL TUBE DEFECTS***
Ethosuximide***
- MOA: inhibits low-voltage activated T-type Ca2+ channels in thalamocortical neurons
- used for generalized ABSENCE SEIZURES** (1st line)
- AE: EFGHIJ -> fatigue, GI distress, headache, itching, SJS
AE of Lamotrigene
-insomnia, somnolence, skin rash
Tiagabine
- MOA: inhibitor of GAT-1 GABA transporter preventing uptake
- AE: DIZZY, DROWSY, NERVOUSNESS, LACK CONCENTRATION***
Vigabatrin
- MOA: inhibits GABA-T -> prevent breakdown
- AE: PERMANENT VISUAL LOSS**
Levetiracetam***
- MOA: unknown; binds to SV2A (vesicle membrane protein) reducing release of glutamate
- one of the MOST COMMONLY prescribed drugs for epilepsy**
- few AE -> personality change, fatigue, drowsy, headache
Gapapentin
- MOA: binds alpha-2-delta1 Ca2+ channels
- AE: somnolence, ataxia
Ezogabine (retigabine)
- MOA: allosteric binds KCNQ K+ channels
- AE: PIGMENT DISCOLORATION of RETINA and SKIN***
drug that treats focal seizures in elderly
lamotrigine
- also used as mono therapy for focal seizures
- blocks Na+ and R-type Ca2+ channel & activates HCN K+ channel
Phenobarbital
- MOA: allosteric modulators of GABAa at low concentrations and directly binds to GABAa at high concentrations
- used in status epilepticus (2nd line)
- hepatotoxic, obstruct airway, porphyria, CNS depression
drugs that block AMPA/kainate receptors
topiramate and perampanel
-allosteric antagonists
drugs that inhibit carbonic anhydrase isoenzymes 2 and 4
Topiramate and Zonisamide
