Smoking Cessation

SMOKING CESSATION "Cigarette smoking... .is the chief, single, avoidable cause of death in our society and the most important public health issue of our time." There are an estimated 4,800 compounds in tobacco smoke ---NAIL POLISH REMOVER ACETANISOLE ACETIC ACID АCЕTONE ACETOPHENONE ALFALFA EXTRACT ALLYL IONONE ALMOND BITTER OIL ALUMINIUM AMMONIA - - HOUSEHOLD CLEANER AMMONIUM BICARBONATE AMMONIUM SULFIDE ARSENIC RAT POISON BENZALDEHYDE GLYCERYL BERYLLIUM (METAL) BUTANOL BUTANE CADMIUM CAFFEINE - RECHARGABLE BATTERIES CALCIUM CARBONATE CARBON DIOXIDE CARBON MONOXIDE CITRONELLA OIL CHLOROFORM COCONUT OIL COFFEE CAR EXHAUST CUMINALDEHYDE CYANIDE CYESTINE DANDELION ROOT EXTRACT DAVANA OIL DDT/DELDRIN– EUCALYPTOL GAS CHAMBERS PESTICIDES FARNESOL FENCHONE FENNEL SWEET OIL FIG JUICE FORMALDEHYDE LACTIC ACID EMBALMING FLUID - - - -· PENCILS LEAD MACE POWDER EXTRACT MENTHOL NICOSAMINES PATCHOULI OIL POLONIUM-120 RADIOACTIVE AGENT PANGER RUM ETHER SILICON SKATOLE SMOKE FLAVOR URINE SNAKEROOT OIL UREA As early at 1988, a report from the U.S. Surgeon General stated: The pharmacologic and behavioral processes that determine tobacco addiction are similar to Nicotine is the Cigarettes and other forms of tobacco drug in tobacco that causes those that determine addiction to drugs such as heroin and cocaine are addicting addiction Nicotine is an addiction, with all of the associated pathophysiology, not simply a habit PHARMACOLOGY PHARMACOKINETICS: the effects that the body has on a drug-specifically, the drug's absorption, distribution, metabolism, and excretion PHARMACOKINETICS Nicotine, composed of a pyridine ring and a pyrrolidine ring, is one of the few natural alkaloids that exists in the liquid state. Nicotine is a clear, weak base (pka = 8.0) that turns brown and acquires the characteristic odor of Nicotine is a weak organic base (pka = 8.0): @ pH = 10 @ pH = 8 O pH = 7 @ pH = 6 Pyrrolidine ring 99% unionized /1% ionized 50% unionized / 50% ionized tobacco following exposure to air. 10% unionized / 90% ionized Pyridine ring 1% unionized / 99% ionized CH, IN ACIDIC IN NICOTINE CHEMISTRY ALKALINE » Nicotine is largely ionized and therefore MEDIA poorly absorbed pH MEDIA | across membranes Nicotine is well absorbed in the small intestine but has low Nicotine is readily absorbed » Nicotine is largely unionized and therefore well absorbed across membranes » At physiologic pH (7.3-7.5) in lung tissues - 31% of nicotine is unionized and is readily absorbed through intact skin bioavailability (30%) due to first-pass hepatic metabolism » Tobacco companies buffer products with ammonia purposefully in order to enhance nicotine absorption (or perhaps maliciously in order to promote addiction). IN ACIDIC MEDIA (significant absorption) pipes, cigars, spit tobacco, oral nicotine products SKIN IN ALKALINE MEDIA GI (limited absorption) cigarettes Nicotine is "distilled" from burning tobacco and carried in tar droplets Onset of action is rapid, with inhaled nicotine reaching the brain approximately 11 seconds following inhalation... Rapid onset and high levels of nicotine in the central nervous system produce an almost immediate effect. This Nicotine is rapidly absorbed across respiratory epithelium coupled with a rapid decrease in CNS levels of nicotine reinforces the behavioral act The characteristics of pulmonary tissue that aid absorption include: of smoking stimulates repeated administration. TISSUE > pH of the lung is 7.4 > Surface area of alveoli is large > Capillary system in lung is extensive 10-20% excreted Daily dose of nicotine (in mg) = plasma cotinine concentration (ng/mL) x 0.08 Example: An average cotinine concentration of 300 ng/mL in a typical smoker corresponds to a daily intake of 24 mg unchanged in urine 70-80% cotinine w 10% other 20 10 1 2 3 4 5 6 7 89 10 Metabolized and excreted in urine Minutes after light up of cigarette Nicotine Metabolism nicotine. A smoker absorbs, on average, approximately 1 mg of nicotine per cigarette. It can then be estimated that a Half-life plasma cotinine level of 300 ng/mL corresponds to a daily intake of 24 cigarettes. 300 ng/mL x 0.08 = 24 mg = 24 cigarettes (1 mg = 1 cigarette Nicotine t2 Cotinine t2 02 00 00 19 00 00 Excretion Occurs through kidneys (pH dependent; + with acidic pH) Through breast milk Nicotine Excretion PHARMACODYNAMICS: the effects of a drug on the body PHARMACODYNAMICS Nicotine binds to nicotinic + cholinergic receptors in the brain Pleasure Arousal, enhanced vigilance Improved task performance Anxiety relief Pancreatic I Inflammation Increased metabolic rate Appetite -I Suppression Skeletal Muscle Relaxation Increase Heart rate Increase Cardiac output Increase Blood pressure Coronary vasoconstriction Cutaneous vasoconstriction NOCOTINE ABSORBTION