07 Caffeine and Nicotine

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Oct 30, 2023

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Caffeine and Nicotine Chapter 6
Caffeine Most widely consumed psychoactive drug in world Stimulates the CNS and cardiac muscle Occurs naturally Coffee bean Tea leaf Kola nut Cocoa bean
Caffeine - Pharmacokinetics Absorption Rapidly and completely absorbed Onset of effects felt between 15-20 mins 99% is absorbed in 45 min Distribution Soluble in water and lipids Freely crosses the BBB Metabolism In liver by CYP-1A2 Active metabolites Theophylline Paraxanthine Theobromine (not similar) Certain SSRIs are inhibitors of CYP-1A2 Excretion Primarily through urine half-life varies from about 2.5 to 7 hrs.
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Caffeine - Mechanism of Action Adenosine is Inhibitory Caffeine blocks these receptors Neuromodulator DA, Norepinephrine, Glutamate, Acetylcholine Diffuse system How it works Naturally, levels increase during day Exert a sleep-inducing effect Caffeine weakens effect promotes wakefulness
Beneficial Effects of Caffeine Coffee Cardiovascular function Gastrointestinal Cancer Neurological Cognition and mental health Other physiological actions
Adverse Effects of Caffeine Heavy Consumption 12 or more cups per day, or 1.5 grams of caffeine Agitation, anxiety, tremors, rapid breathing, and insomnia Lethal Dose Estimated at 10 grams taken orally (about 100 cups of coffee); death is due to convulsions and respiratory collapse; six deaths in humans
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Energy Drinks Have caffeine content that may be categorized as “natural” content and not FDA regulated Involved in more than half of U.S. poison control center calls involving children under 6 years Caffeine and Alcohol Enhances alcohol tolerance Counteracts some symptoms of hangover Masks some cues of intoxication
Tolerance and Dependence Some Effects Become Tolerant in Humans Blood pressure, heart rate Sleep disturbances Anxiety, nervousness, energy More likely with high doses (750 to 1200 milligrams) Some Effects that Did Not Show Tolerance Caffeine-induced alertness and wakefulness Cerebral energy metabolism Withdrawal Headache (most common) Drowsiness Fatigue Negative mood Drug craving
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The effects of Nicotine What are the risks? Tobacco is the leading cause of preventable death and disease in the US Adverse effects: Clotting and strokes Cardiovascular disease Cancer Respiratory tract infections Fetal effects The good and bad news? Quitting can reverse a lot of the damage done 6% successful at quitting
Nicotine: Pharmacokinetics More than 4000 compounds released during smoking The 3 most important compounds in smoke Carbon Monoxide Tar Nicotine 8-10 mg in an average cigarette Average smoker absorbs 2-2.5 mg per cigarette Absorption and Distribution Quickly from many sites Lungs Mucous membranes of mouth and nose Skin Distributed to Brain Metabolism Liver 80-90% Cotinine Half-life ~ 2-4 hours Excretion Urine Saliva and Sweat
The rewarding effects of Nicotine Stimulate nicotinic acetylcholine receptors (nAChRs) - So it is an agonist Activation of nicotinic receptors on neurons in the VTA causes DA release onto the nucleus accumbens. Activation of nicotinic receptors on neurons in the frontal cortex causes glutamate to be released onto VTA. Nicotine desensitizes nicotinic receptors on VTA neurons that release gamma aminobutyric acid (GABA), leads to increased DA release in the VTA
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