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ethyl alc


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Alcohol oxidation pharmacokinetics
1)zero-order kinetics - constant amount is oxidized at a constant rate; metabolism independent of time or conc of alcohol in body
Typical adult metabolizes how much alcohol per hour?
7-10grams of alcohol per hour
Pathways that alcohol is metabolized
1)alcohol dehydrogenase (liver) producing acetaldehyde
2)microsomal ehtanol oxidizing system (MEOS)
-chronic alcohol consumption induces microsomal enzyme system
role of aldehyde dehydrogenase
acetaldehyde -> acetate -> H2O + CO2
MOA of antabuse (disulfiram)
1)inhibits aldehyde dehydrogenase
alcohol and antabuse used together
severe reaction consisting of headache, nausea, flushing, confusion
graded depression of CNS with alcohol
release of inhibitions -> anxiolytic effect -> sedation -> hypnosis -> anesthesia -> respiratory depression -> coma -> death
High doses of alcohol effect
depress respiration and may cause respiratory arrest
management of acute alcohol intoxication
1)main goal is to prevent or treat severe respiratory depression
2)prevent aspiration of vomitus
Ohter actions of alcohol
1)HTN, cardiomyopathies, arrhythmias (chronic use)
2)inhibits secretion of ADH
3)stimulates gastric acid secretion
4)stimulate appetite (small amts); suppress appetite (large amts)
6)anemia, folic acid deficiency
7)gynecomastia, testicular atrophy
Management of alcohol withdrawal
1)main objective is to prevent SZRs, delirium, and arrhythmias
2)BZDs (lorazepam, oxazepam, diazepam)
3)phenytoin (control SZRs)
4)beta blockers, clonidine alleviate automonic effects
5)vitamin supplementation (thiamine)
6)antipsychotics for hallucinations may increase risk of SZRs
Management of alcohol dependence after withdrawal
1)NALTREXONE (long-acting opiod antagonist) reduce craving for alcohol
2)ACOMPROSATE decrease craving and help maintain abstinence (possible MOA may involve actions at both glutamate and GABA receptors
MOA of morphine/opiods
agonist at receptors for endogenous opiod peptides (endorphins and enkephelins) and modifies the processing of pain information in CNS
mu receptor effects
1)respiratory depression
4)suprespinal analgesia
kappa receptor effects
4)spinal analgesia
delta receptors effects
morphine effects at receptors
1)strong agonists at mu
2)moderate agonists at kappa
3)weak agonists at delta
pentazocine effects at receptors
1)strong agonists at kappa
2)partial agonists or antagonists at mu receptors
naloxone effects at receptors
1)antagonist at all types of opiod receptors
what type of receptor agonists have the highest abuse potential
mu agonists
morphines analgesia effects
1)limbic system (modify patient's rxn to pain)
2)spinal cord (modify physiological sensation of pain)
what types of pain is morphine most effective
dull, constant, visceral pain
difference between opiates and non-opiates at therapeutic doses
morphine does not cause loss of consciousness which differs from non-opiate drugs
other effects of morphine/opiods
1)nausea (tolerance develops)
2)respiratory depression (usual cause of death in opiod poisoning-dec sensitivity to CO2 at chemoreceptors in medulla)
3)miosis (pin-point pupils)
4)antitussive effect
5)constipation/urine retention
7)increased biliary pressure
8)orthostatic hypotension
9)cutaneous vasodilation
10)increased CSF pressure
standard therapeutic dose of morphine
10mg SC or IM
medications that can enhance the effects of opiods
1)antihistamines (hydroxyzine)
Examples of strong mu agonists
morphine, codeine, hydromorphone, oxymorphone, levorphanol, oxycodone, hydrocodone, meperidine, heroin, methadone, levo-alpha-acetylmethadol, propoxyphene, fentanyl, sufentanil, alfentanil
Meperidine characteristics
1)1/10 potency of morphine
2)less constipation and urine retention
3)used for mod-sev pain
4)used in obstetrics (less respiratry depression in newborn than morphine)
5)active metabolite that can cause SZRs (not for chronic pain)
methadone characteristics
1)less euphoric
2)longer duration of action (12-24hr) than heroin (2-4hr) or morphine (4-6hr)
3)used as analgesic (4-6h) and in treating opiod addiction (24hr)
drugs that can induce neuroleptic analgesia
fentanyl plus droperiodol (Innovar)
-used for diagnostic and minor surgical procedures
drugs that can induce neuroleptic anesthesia
Innovar plus nitric oxide
these agents are similar to fentanyl but used I.V. as adjuncts for surgical anesthesia
sufentanil and alfentanil
percocet components
opium tincture characteristcs
10mg morphine per mL
-orally for mild pain or diarrhea
paregoric characteristics
2mg morphine per 5mL
pentazocine (Talwin) characteristics
1)agonist at kappa receptors, partical agonist at mu receptors
2)mu antagonist at high doses
3)CNS stimulation and hallucinations more common than w/ morphine
4)less sedation and respiratory depression than w/ morphine
buprenorphine characteristics
1)partical agonist at mu receptors, possibly kappa receptors
2)used for opiod dependence
3)reduce craving in heroin addicts
Suboxone components
-high doses, naloxone blocks effects of buprenorphine
tramadal (Ultram) characteristics
1)weak mu agonist
2)inhibits synaptic uptake of NE and 5-HT
3)used for mild-mod pain
drug of choice for opiod poisoning-can reverse respiratory depressant effects of opiods
-must be given parenterally
-short acting (2hr)
naltrexone characteristics
-long acting (24hr)
-immunizes addicts (prevents high)
-patient must be detoxified
-treatment of alcoholism
opiod poisoning symptoms-characteristic triad
1)CNS depression-stupor or coma
2)depressed depth and rate of respiration
3)pin point pupils (may be dilated if severely hypoxic - close to death)
treatment of opiod poisoning
1)support respiration (O2 administration may remove hypoic drive or respiration and cause apnea)
duration and intensity of actue withdrawal
1)short acting drug (heroin)
-intense sxs, short duration (2-3d)
2)long acting drug (methadone)
-moderate sxs, long duration (4-7d)
3)followed by prolonged syndrome of mild anxiety, irritability, sleep disturbances, autonomic excitability that may last for several weaks-months
treatment of opiod dependence

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