Exam 2 Flashcards
Methadone (Dolophine)
Strong opioid agonist
Orally effective
Longer duration of action
Used for detoxification and controlled withdrawal from heroin and morphine
Codeine
Moderate opioid agonist
Metabolized to morphine for analgesic activity
Used with aspirin and acetaminophen for moderate pain
Included in many cough syrups for relief of cough
0.5% concentration in opium
Pentazocine (Talwin)
Mixed opioid agonist-antagonist
A kappa-receptor agonist with weak mu-receptor antagonist activity
Orally administered for treating moderate to severe pain
Parenteral formulation as a preanesthetic medication
Precipitates a withdrawal syndrome in a morphine abuser
Buprenorphine (Buprenex)
Mixed opioid agonist-antagonist
A partial agonist at mu-receptors and an antagonist at kappa-receptors
Resistant to naloxone reversal
Used to manage cocaine addiction and heroin abuse
Naloxone(Narcan)
Opioid antagonist
A competitive antagonist (half life time is 1-2 hours)
No obvious effects in normal people
Antagonist-precipitated withdrawal
Intravenous injection for treating opioid overdose
Naltrexone (ReVia)
Opioid antagonist A competitive antagonist (half life time is 10 hours) Antagonist-precipitated withdrawal A "maintenance" drug for addicts Also used in treatment of alcoholics
Carbamazepine (Tegratol)
Enhance Na+ channel inactivation
P450 inducer (1/2 life shortens from 36 hr to 8-12 hr with chronic treatment)
Common adverse reactions: diplopia, ataxia, drowsiness
Tegratol-XR sustained release form
Used also for neuropathic pain, bipolar disorder
Induces metabolism of other drugs
Topiramate (Topomax)
A D-fructose analog
Multiple mechanisms of action: blocks Na channels, increases affinity of GABA for its receptors, blocks AMPA-type glutamine receptors
1/2 time = 21 hr; mostly excreted unchanged in urine
Broad spectrum anticonvulsant, widely used
Common adverse reactions: sleepiness, dizziness, balance issues, often resolve over time
Also used for migraine prophylaxis
Ethosuximide (Zarontin)
Block Ca channels Drug of choice for absence epilepsy T-type Ca channels not involved in transmitter release No plasma protein binding 1/2 life 40-60 hrs with renal excretion
Valproate (Depakote)
Enhance GABAergic inhibition
Broad spectrum anticonvulsant
Divalproex Na is a sustained release form
Hepatotoxicity - contraindicated in hepatic disease and children less than 2 yrs
Mixed mechanism: also blocks Na channels
Also used for bipolar disorder and migraine prophylaxis
Inhibits metabolism of other drugs and is highly protein bound
Levetiracetam (Keppra)
Mechanism of action: SV2A target
Most common type of seizure affected: partial complex
Tiagabine (Gabitril)
Mechanism of action: potentials GABAergic inhibition
Most common type of seizure affected: partial complex
Clozapine (Clozaril)
Parkinson’s disease therapy #1: replace the lost dopamine (L-DOPA, cabidopa)
D2 antagonist active on mesolimbic dopamine receptors, can blunt psychotic effects such as hallucinations, delirium, depression, sleep disturbances
Bromocryptine (Parlodel)
Parkinson's disease therapy #2: Directly activate dopamine receptors in striatum Prototype, a D2 agonist Greater than 90% 1st pass metabolism 3 hour 1/2 life
Cabergoline (off label)
Parkinson’s disease therapy #2:
Directly activate dopamine receptors in striatum
Has 66 hr 1/2 life
2x/week PO
Ropinirole (Requip)
Parkinson’s disease therapy #2:
Directly activate dopamine receptors in striatum
Causes fewer dyskinesias than L-DOPA
Often used intitially, or in combo with L-DOPA
Adverse effects: nausea, mental confusion, hallucinations
Selegiline (Eldepryl)
Parkinson’s disease therapy #3:
Scavenge free radicals and inhibit MAO-B
Prototype
Tetrabenazine (Xenazine)
Huntington’s disease
Approved in 2008: VMAT2 inhibitor that depletes dopamine; reduces dyskinesias but not cognitive seizing or mood issues
Might also be useful for tardive dyskinesias
Lidocaine
Amide
The most broadly used local anesthetic
Intermediate duration (approx 2 hr spinal, 30-60 min for topical or infiltration)
Higher systemic toxicity than ester-linked drugs
Metabolized by liver
Uses: spinal, epidural, local, topical
Careful: concurrent use with amiodarone
Procaine (Novocaine)
Ester Introduced in 1905 Short acting (40 sec plasma 1/2 life) Low toxicity Main use: infiltration and regional anes Interaction: PABA blocks sulfonamide action
Tetracaine (Pontocaine)
Ester
Intermediate duration of action (slowly hydrolyzed: 2 hr spinal anes, 30-60 min for topical)
Higher systemic toxicity than other esters
Tends to cause mucous membrane irritation, uticaria, burning
Main uses: spinal & topical anes of nose and throat for diagnostic procedures
Bupivacaine (Marcaine)
Amide
Widely used local anesthetic
Long duration of action (3-9 hr regional anes, plasma 1/2 life 3.5 hr adult, >8 hr neonate)
Concurrent epidural use with opiates in labor can reduce the amount of opiate needed for analgesia
More cardiac effects than lidocaine due to slower dissociation from cardiac Na channels
Synergistic with anti-arrhythmics on heart - can induce arrhythmias (treatment: iv admin of lipid emulsions)
Morphine
Strong opioid agonist
4-6 hour duration of action
Active metabolite: morphine-6- glucuronide
Treatment of severe pain associated with trauma, myocardial infarction, and cancer
Major active ingredient in opium (10%)
