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21 Cards in this Set
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Sedative/hypnotic. Useful for methanol toxicity. Interacts allosterically with GABAa receptor to facilitate GABA mediated opening of chloride channels and inhibition of neuronal activity.
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Ethanol
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Metabolized by Alcohol Dehydrogenase and MEOS (saturated after 1 drink/hour. MEOS induced by chronic alcohol use. Metabolized to ACETALDEHYDE (toxic).
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Special populations that Ethanol has different effects on.
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Women and Asians.
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Women have a less active form of gastric ADH. Asians have a modified form of ADH, causing facial flushing and headaches.
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Acute actions of Ethanol.
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Depression of myocardial contractility, cutaneous vasodilation due to inhibition of the vasomotor thermoregulatory center (profound hypothermia), diuresis due to inhibition of ADH release and increased plasma fluid volume.
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Chronic actions of Ethanol
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Thiamine deficiency (vit B1), decreases transketolase activity with pyruvic acid accumulation, causing neuron damage. WKS. REDUCES RISK OF CARDIOVASCULAR DISEASE (increased HDL and antioxidant action).
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Drug Interactions of Ethanol
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Benzo's (additive CNS Depressant Activity), Warfarin (inh's metabolism at high doses)
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Inhibits aldehyde dehydrogenase.
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Disulfiram (Antabuse)
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adjunct in the treatment of alcoholism. DO NOT DRINK EtOH!!! Can't tolerate.
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Opioid receptor antagonist. Reduces craving for specific substance.
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Naltrexone (alcoholism tx)
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Competitive inhibitor of NMDA glutamate recepetor to reduce craving for
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Acampraosate (alcoholism tx)
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Blocks DA transporters (extends life of extracellular DA and NE).
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Cocaine
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Metabolized by plasma and liver cholinesterase. Extraordinary tolerance.
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Increases release of catecholamines in the CNS (DA and NE), inhibits MAO. Direct sympathomimetic actions.
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Amphetamine/Methamphetamine
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Extraordinary tolerance. SE (same for cocaine): anxiety, tachycardia and hypertension, sexual dysfunction, seizures (from hypothermia or seizure threshold), coronary vasospasm, arrhythmia, MI, hallucinations, NECROTIZING ARTERITIS with renal failure or GI necrosis (with Amphetamines).
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Amphetamine Analogue for ADHD. Can also be used for Narcolepsy.
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Methylphenidate (Ritalin)
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reduces behavioral problems, aggression, noncompliance and negativity
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Mimics ACh. Increases release of NE and Epinephrine from the adrenal glands, and ACh, NE, DA, and 5-HT in the CNS.
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Nicotine
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Increases release of ADH, causing fluid retention. Metabolized in liver by CYP2A6 to inactive Cotinine. t1/2 is 2 hours. CELLULAR TOLERANCE (adaptation of neurons). Strong PSYCHOLOGICAL dependence.
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Withdrawal to this substance is characterized by a sharp decline in DA levels in the Nucleus Accumbens. Occurs after 24 hours and persists for weeks to months.
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Nicotine
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"craving" is a sign of psychological dependence.
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Chewing gum used to prevent withdrawal symptoms for cigarettes.
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Nicotine Polacrilex
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Compliance is poor.
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The preferred therapeutic modality for cigarette withdrawal
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Nicotine Transdermal Patch
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Most common problem is local skin irritation.
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Two Non-Nicotine therapies to manage withdrawal.
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Bupropion (antidepressant) and Verenicline (nicotine receptor partial agonist).
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Second line therapies.
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delta-9 tetrahydrocannabinol G-Protein receptors. Indicated for use in N/V cases from chemo and AIDS. Decreases IOP in glaucoma. Decreases neuropathic pain.
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Marijuana (THC)
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THC analogue. Amelioration of nausea and vomiting. Appetite stimulant.
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Dronabinol
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Hallucinogen. Direct partial agonist of 5-HT receptors.
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LSD, Lysergic Acid Diethylamide
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Dilated pupils, increased BP. Tx with Benzos and "talking down."
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Antagonist at glutamate NMDA recepetors. Dissociates individuals from themselves and environment.
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PCP, Phencyclidine
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Hallucinogen. Tx: induced vomiting, respiratory support, seizure control with BZ, reduce sensory stimulation.
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For ethylene glycol poisoning. Inhibits alcohol dehydrogenase.
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Fomepizole. Alcohol can be used, too.
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