Pharm 30 Opiods, Alcohol, Barbituates And Benzos

Front 1

Heroine:
1) What is it?
2) Where is it?
3) Mechanism of action?

Back 1

1) Diacetyl morphine
2) Quickly crosses BBB and is converted to monoacetyl morphine --> morphine
3) Binds directly and rapidle to opioid mu, delta, and kappa receptors

Front 2

Heroine: Routes of administration and timing of peak effect
1) Intranasal (snorting) and intradermal (skin popping)
2) IV (mainlining) or inhalation
3) What is it mixed with and what are risks?

Back 2

1) 5min
2) 1-5 min
3) Starch, sugar, powdered milk, poisons, quinine, strychnine --> risk of OD

Front 3

Heroine: Immediate drug effect

Back 3

-rush
-analgesia
-drowsiness
-unconsciousness
-respiratory depression
-pupil constriction
-flushing of skin
-itching
-nausea and vomiting
-spontaneous abortion

Front 4

Heroine: Withdrawal sxs

Back 4

-piloerection
-rhinorrhea
-yawning
-persperation
-lacrimation
-mydriasis
-tremors
-wt. loss
-m. twitches
-restlessness
-vomiting
-hot and cold flashes
-abdominal cramps
-anxiety: benzos (clonazepam/oxazepam)
-diarrhea
-severe cramping: benzos (clonazepam/oxazepam)
-insomnia: benzos (clonazepam/oxazepam)

Front 5

Heroine: txt of withdrawal symptoms
1) Insomnia, anxiety, muscle spasm
2) Muscle and bone pain
3) Nausea, vomiting
4) Mydriasis/alpha 2 antagonists
5) Diarrhea

Back 5

1) Benzos (clonazepam, olanzepam
2) NSAIDS, ketorolac
3) Antimimetics (ondansetron, prchlorperazine)
4) Reduce sympathetic hyperactivity via feedback inhibition (clonidine, guanfacine, lofexidine)
5) Anti-diarrheal agents: loperamine, octerotide (analog of sandostatin)

Front 6

Methodone
1) What is it used for?
2) Mechanism
3) Dosing, administration
4) Half life
5) Caution
6) Use for pain?

Back 6

1) Maintenance for heroine
2) agonist, prevents heroin effects be producing tolerance
3) Must be >70mg/day oral
4) 15-40hrs
5) More than 40mg in nontolerant individual -->respiratory depression and death
6) Dangerous in patients without opioid tolerance.

Front 7

LAAM
1) Drug class and use

Back 7

1) Opioid agonist, used for heroine txt

Front 8

Buprenorphine
1) Drug class
2) Uses
3) Advantages over agonist
4) Affinity for receptors

Back 8

1) Partial mu agonist and kappa antagonist
2) Heroine maintenance
3) With increased dosing no increased risk for respiratory depression just increase in duration
4) High affinity for mu --> displaces morphine and methadone and out competes naloxone (--> prevention of withdrawal)

Front 9

Buprenorphine Pharmokinetics
1) Administration, dosing
2) Duration of effect
3) Metabolism
4) Inhibitors of metabolism
5) Inducers of metabolism

Back 9

1) Sublingual tablet F= 70% (poor oral bioavailability). Low does may not fully block reinforcing effects of heroine
2) Very slow dissociation from mu R --> dosing every other day
3) Cyt p450 3A4
4) grapefruit juice, SSRIs, some antiinfectious agents, calcium channel blockers, some retrovirals
5) Anti-epileptics (carbamazepine, phenytoin, phenobarbitol), anti-TB, rifampin

Front 10

Buprenorphine: Abuse potentials
1) Non-dependent opioid users
2) Physically dependent opioid users

Back 10

1) Does produce euphoria, mostly via IV, not abused very often
2) Can precipitate with drawal: higher doses of drug more likely to precipitate withdrawal. Also should be given 36 hrs after methadone to prevent withdrawal.

Front 11

Buprenorphine: ORL-1

Back 11

Site of action unique to buprenorphine, actions unclear. May relate to diminished respiratory depression, alertness, and mood.

Front 12

Naltrexone
1) Drug class
2) Use
3) Administration
4) Effectiveness

Back 12

1) Mu antagonist
2) Heroine maintenance therapy
3) Oral table, 1X per day for month
4) Not very, high drop out rate because precipitates withdrawals in physically dependent people, best in high pressured situations when pt has been off opioids for at 5-7 days.

Front 13

Alcohol
1) Mechanism of action
2) Acute effects on CV, UG, sexual function

Back 13

1) Proposed: enhancement of GABA, inhibition of Ca conductance and/or gluatamate receptors
2) CV- cutanious vasodilation, may decrease risk of MI due to increased HDL and decreased platelet aggregation. UG- Inhibits ADH release. Sexual function decreased

Front 14

Alcohol: Chronic effects
1) Liver
2) Fetal alcohol syndrome
3) What other systems does it effect

Back 14

1) Fatty deposition --> cirrhosis
2) Increased stillbirths and spontaneous abortions in women that drink 2-3 drinks a day. Lowest concentration of alcohol to produce FAS = 2.5 oz pure or 6.5 oz spirits

Front 15

Alcohol: Withdrawal sxs
1) 5-10 hr. post last drink
2) 24 hrs post last drink
3) Sever withdrawal

Back 15

1) Tremor, increased pulse, respiration, temperature, sweating, insomnia, bad dreams, GI upset, nausea, anorexia
2) Siezures (rum fits), grand mal
3) Delirium tremens (DT) <5%, 3-7 days post last drink, more likely with intercurrent medical illness --> delirium/confusion, hallucinations, autonomic dysfunction inc. fever, and elevated vitals, Mortality = 10-15%

Front 16

Naloxone
1) Mechanism of action
2) Sublingual bioavailability --> implications
3) IV effects, Administration and why
4) Half life

Back 16

1) Bind tightly to opioid receptors
2) Poor, 1-2 mg produces no withdrawal effects and when used 1:4 combo with buprenorphine, mostly buprenorphine effect induced
3) If opioid dependent person tries to abuse buprenorphine by administering it IV, naloxone effect with dominate --> withdrawal syndromes
4) Very short

Front 17

Alcohol: Detoxifiction
1) Where?
2) Switch to what?
3) What other supportive txt?

Back 17

1) Hospital often
2) benzos then taper off
3) Nutritional supplementation, bridge to treatment, psychosocial

Front 18

Disulfram
1) Use
2) Mechanism of action
3) Effect proportional to what
3) Resultant sxs

Back 18

1) Antabuse for alcohol
2) Irreversiblty inhibits ADH, aldehyde dehydrogenase --> great increase (5x normal) levels of acetaldehyde alcohol metabolite.
4) Both alcohol and dose of disulfram, persists as long as alcohol is metabolized
3) flushing, headache, respiratory difficulty, nausea, vomiting, sweating, thirst, chest pian, vertigo, orthostasis, potentially death
4) Compliance,

Front 19

Naltrexone
1) Mechanism
2) Behavioral actions
3) Problem

Back 19

1) Antagonist to opioid receptor, prevents effects of alcohol
2) Studies shows diminishes relapse/excessive drinking
3) compliance