Term
Opioid analgesics
Mech
Use
Tox |
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Definition
Morphine, Fentanyl, Codeine, Heroin, Methadone, Merperidine, Dextromethorphan
Agonists at mu opiod receptors, open K channels, close Ca channels, decrease synaptic transmission.
Pain, cough suppression, diarrhea, acute pulmonary edema, maintenance for addicts
Addiction, resp. depression, constipation, miosis, additive CNS depression, sphincter of Oddi tone - pancreatitis. Tolerance does not develop to miosis and constipation.
Treat tox. with naloxone or naltrexone (opiod receptor antagonists) |
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Term
Meperidine
Class?
Special use? |
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Definition
Opioid
Less sphincter of Oddi effect - usable in pancreatitis. |
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Term
Loperamide
Class?
Special use? |
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Definition
Opioid
Anti-diarrhea (imodium) |
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Term
Diphenoxylate
Class?
Special use? |
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Definition
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Term
Dextromethorphan
Class?
Special use? |
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Definition
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Term
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Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
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Term
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Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
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Term
Buprenorphine
Mech
Use?
Tox? |
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Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
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Term
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Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
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Term
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Definition
Partial agonist of mu opioid receptors, agonist at kappa receptors,
Pain, less resp. depression than full agonists.
Causes withdrawal if currently on full agonist. |
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Term
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Definition
Very weak opioid agonist; also inhibits 5-HT and NE reuptake.
Chronic pain.
Some opioid toxicity, decreases seizure threshold. |
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Term
| Drugs of choice for tonic-clonic seizures? Mechanism? |
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Definition
Phenytoin, Carbamazepine, Valproic acid (1st)
Lamotrigine, Topiramate (2nd) Block Na channels |
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Term
Drugs of choice for partial seizures?
Mechanism? |
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Definition
Gabapentin, Tigabine, Vigabatin, Levetiracetam, Phenobarbital, Benzodiazepines
All increase GABA action by various mechanisms. |
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Term
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Definition
Na channel inactivation
Tonic-clonic seizures, *prophylaxis/prevent recurrence of status epilepticus, *class IB anti-arrythmic
Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsuitism, lymphadenopathy, megaloblastic anemia, teratogenesis. Drug induced-SLE, P450 induction. Also P450 metabolized. |
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Term
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Definition
Na channel inactivation
Tonic-clonic seizures, trigeminal neuralgia.
Diploplia, ataxia, *agranulocytosis, *aplastic anemia, liver toxicity, teratogenesis, P450 induction, SIADH, Stevens-Johnson syndrome.
NB: Oxcarbamazepine: same use, fewer AEs |
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Term
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Definition
Blockes voltage-gated Na channels
Tonic-clonic seizures
Stevens-Johnson syndrome |
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Term
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Definition
Designed as GABA analog, but mainly blocks Ca channels
Partial seizures, tonic-clonic seizures, peripheral neuropathy, bipolar disorder
Sedation, ataxia |
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Term
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Definition
Blocks Na channels, increases GABA action
Partial seizures, tonic-clonic
Sedation, mental dulling, kidney stones, weight loss |
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Term
|
Definition
Phenobarbital, pentobarbital, thiopental, secobarbital
Increases GABA action by increasing duration of Cl channel opening
Partial seizures, tonic-clonic, *1st line in pregnant women, children.
Anxiety, insomnia, anesthesia induction Sedation, tolerance, dependance, induces P450. Contraindicated in porphyra (stimulate ALA synthase) |
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Term
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Definition
Inactivates NA channels, increases GABA concentration
Tonic-clonic (1st), partial, myoclonic, bipolar disorder, *also tonic-clonic + absence
GI distress,
*rare but fatal hepatotoxicity, neural tube defects (CI: preg), tremor, weight gain. |
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Term
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Definition
Blocks thalamic T-type Ca channels
Absence seizures (1st)
GI distress, fatigue, headache (EFGH), uticaria, Stevens-Johnson syndrome |
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Term
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Definition
Inhibits GABA reuptake
Partial seizures only |
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Term
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Definition
Irreversibly inhibits GABA transaminase, raising [GABA]
Partial seizures only |
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Term
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Definition
Unknown, may modulate GABA and glutamate release
Tonic clonic, partial |
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Term
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Definition
Blocks voltage gated Na channels and T-type Ca channels
Partial, Tonic-Clonic, Absence |
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Term
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Definition
Blocks glutamate at NMDA
Partial and Tonic-Clonic; less use b/c toxicity
aplastic anemia, hepatotoxicity |
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Term
| Drugs acting on GABA-A receptor? |
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Definition
Barbituates, benzodiazepines, alcohol.
An ion channel, GABA increases Cl infux. |
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Term
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Definition
Baclofen (muscle relaxant)
Gi receptor. Inhibits adenylyl cyclase, K efflux, Ca influx. |
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Term
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Definition
ion channel, allows Cl influx.
No drugs active here. |
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Term
Benzodiazepines
Mech
Use
Tox
Antidote |
|
Definition
"pams" and "lams": Diazepam, Lorazepam, Triazolam, Temazepam, Oxazepam, Midazolam, Alprazolam &* chlordiazepoxide.
Increase frequency of Cl channel opening at GABA-A receptor.
Anxiety, spasticity, status epilepticus, detoxification (alcohol withdrawal), night terrors (reduces REM sleep), sleepwalking, general anesthetic, hypnotic.
Dependence, additive CNS depression. Less risk of resp. depression and coma than barbituates.
Treat OD with flumazenil (competitive antagonist) |
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Term
| Short acting benzodiazepines? |
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Definition
Triazolam, Oxazepam, Midazolam (TOM thumb)
Greatest addictive potential. |
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Term
Nonbenzodiazepine hypnotics
Mech
use
tox |
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Definition
Zolpidem (ambien), zaleplon, eszopiclone
(ZZZs)
Act on benzodiazepine receptor subtype, reversed by flumazenil.
Insomina.
Ataxia, headaches, confusion. Short duration - hepatic metabolism. Less AEs and dependance than older benzodiazepines. |
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Term
Inhaled anesthetics
Mech
Effects
Tox |
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Definition
"fluranes": Halothane, Enflurane, Isoflurane, Sevoflurane, Methoxyflurane, nitrous oxide
Mechanism unknown!
Myocardial depression, resp. depression, nausea/emesis, increased cerebral blood flow, decreased cerebral metabolic demand
*Hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane), malignant hyperthermia (tx: dantrolene), expansion of trapped gas (NO2) |
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Term
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Definition
PCP analog, blocks NDMA receptor
"dissociative anesthetic". CV stimulant.
Disorientation, hallucination, bad dreams. Increased cerebral blood flow. |
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Term
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Definition
Potentiates GABA
Rapid anesthesia induction for short procedures. |
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Term
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Definition
Depolarizing neuromuscular blocker.
Cannot reverse with cholinesterase inhibitor. |
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Term
Nondepolarizing neuromuscular blocking drugs
names? mech? reversal? |
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Definition
"curarines": Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium.
Competitive for ACh receptors.
Reversable with acetylcholinesterase inhibitor |
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Term
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Definition
Blocks ryanodine receptor on muscle SR
Used in treatment of malignant hyperthermia, neuroleptic malignant syndrome |
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Term
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Definition
BALSAC
Bromocriptine: dopamine agonist
Amantidine: increase dopamine release
L-DOPA/carbidopa: dopamine precursor
Selegiline: MAO-B inhibitor, prevent dopamine breakdown.
Antimuscarinics: Benztropine, best for drug-induced Parkinsonism
COMT inhibitors: entacapone, tolcapone. Prevent L-DOPA degradation |
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Term
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Definition
NMDA receptor antagonist; prevents excitotoxicity
Alzheimer's
Dizziness, confusion, hallucination |
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Term
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Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
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Term
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Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
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Term
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Definition
AChEsterase inhibitor
Alzheimer's
Nausea, Dizziness, insomnia |
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Term
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Definition
5-HT-1B/1D antagonist. Vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release. Halflife < 2hrs.
Acute migraine, cluster headaches.
Coronary vasospasm, (CI: CAD, Prinzmetals) mild tingling |
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Term
Dopamine agonists?
Use?
Classes? |
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Definition
Ergot: Bromocriptine, Pergolide
Nonergot: Pramipexole, Ropinerole
Parkinson's disease, (Bromo: Prolactinoma) |
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