Neurology- Pharmacology Flashcards
Epilepsy drugs
Pag. 528
Eclampsia seizures 1st line treatment
MgSO4
Seizures 1st line in neonates
Phenobarbital (phenoBABYthal)
Phenytoin, fosphenytoin
- Adverse effects
PHENYTOIN: P450 induction, Hirsutism, Enlarged gums, Nystagmus, Yellow-brown skin, Teratogenicity (fetal hydantoin syndrome), Osteopenia, Inhibited folate absorption, Neuropathy
Vigabatrin action mechanism
Irreversible GABA TRansaminase INihibitor:
viGABATRIN
Barbiturates
- Names
- Mechanism
- Clinical uses
Phenobarbital, pentobarbital, thiopental, secobarbital
Facilitate GABA-A action
Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental).
Barbiturates
- Adverse effects
Respiratory and cardiovascular depression; CNS depression (can be exacerbated by alcohol use); dependence; drug interactions (induces cytochrome P-450).
Overdose treatment is supportive (assist respiration and maintain BP). Contraindicated in porphyria
Benzodiazepines
- Mechanism
- Short acting benzoodiazepines
Facilitate GABAA action
Mosthave long half-lives and active metabolites (exceptions [ATOM]: Alprazolam, Triazolam, Oxazepam, and Midazolam are short acting)
Benzodiazepines
- Adverse effects
- Benzodiazepines with liver disease
Dependence, additive CNS depression effects with alcohol. Treat overdose with flumazenil
“OK for Terrible Livers”
Oxazepam, Temazepam, and Lorazepam: they can be used to treat alcohol withdrawal in patients with liver disease due to minimal first-pass metabolism.
Nonbenzodiazepine hypnotics
- Names
- Mechanism
- Clinical use
- Adverse effects
hypnotics Zolpidem, Zaleplon, esZopiclone
Act via the BZ1 subtype of the GABA receptor. Effects reversed by flumazenil. Sleep cycle less affected.
Insomnia
Ataxia, headaches, confusion, low dependence risk.
Suvorexant
- Mechanism
- Clinical use
- Adverse effects
Orexin (hypocretin) receptor antagonist
Insomnia
CNS depression, headache, dizziness, abnormal dreams, upper respiratory tract infection. Contraindicated with strong CYP3A4 inhibitors
Ramelteon
- Mechanism
- Clinical use
- Adverse effects
Melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus.
Insomnia
Dizziness, nausea, fatigue, headache. No dependence
Triptans (sumatriptan)
- Mechanism
- Clinical use
- Adverse effects
5-HT1B/1D agonists. Inhibit trigeminal nerve activation; prevent vasoactive peptide release; induce vasoconstriction.
Acute migraine, cluster headache attacks.
Coronary vasospasm, mild paresthesia, serotonin syndrome
Parkinson disease drugs
BALSA
Bromocriptine, Amantadine, Levodopa (with carbidopa), Selegiline (and COMT inhibitors), Antimuscarinics
Dopamine agonists
Ergot—Bromocriptine.
Non-ergot (preferred)—pramipexole, ropinirole; toxicity includes impulse control disorder, postural hypotension, hallucinations/confusion.
Drugs increasing dopamine availability
Amantadine; toxicity = ataxia, livedo reticularis
Drugs increasing l-DOPA availability (agents act peripheral)
Levodopa (l-DOPA)/carbidopa—carbidopa blocks peripheral conversion of l-DOPA to dopamine by inhibiting DOPA decarboxylase
Entacapone prevents peripheral l-DOPA degradation by inhibiting COMT. Used in conjunction with levodopa.
Drugs: Prevent dopamine breakdown (agents act centrally)
Selegiline, rasagiline—block conversion of dopamine into DOPAC by selectively inhibiting MAO-B.
Entacapone—blocks conversion of dopamine by inhibiting central COMT.
Drugs: Curb excess cholinergic activity
Benztropine, trihexyphenidyl (Antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease).