NSG6005 Advanced Pharmacology Quiz 1|2023 LATEST UPDATE|GUARANTEED SUCCESS

How medication transports through cell Medication (agonists) bind to receptors to elicit response Agonists bind and activate receptor How medication transports through cell Antagonists bind and prevent receptor activation (competitive or noncompetitive inhibition) How medication transports through cell Medications may bind allosterically to another site resulting in an increase or a decrease in the response to the agonist How medication transports through a cell Multiple forms of the same receptors can exist and interact with medications How medication transports through a cell Medications may be bound to proteins How medication transports through a cell Medications may bind to multiple types of receptors resulting in altered therapeutic effects and side effects Ionization Plays a significant role in absorption, distribution across membranes, and renal elimination. Passive diffusion Being charged is a negative factor Primary, secondary, and tertiary amines May take on a charge to become neutral Quaternary amines Always charged Charged medications Water soluble and more easily eliminated by the kidneys Henderson-Hasselbalch equation Defines role of PH t degree of ionization: Log of prontonated=pKa-PH Most drugs Weak acids (donate H+) Weak bases (accept H+) PH of stomach Manipulates base or acid of drug Urine Can alter absorption or elimination based on PH Distribution Requires adequate blood supply. Drug goes to areas of high blood flow first. Areas of low blood supply have a slower delivery Phase I metabolism Oxidation, reduction, deamination, hydrolysis, sulfonation: -OH, -SH, -NH2 added or unmasked. Oxidation The combination of a substance with O2 Reduction The act of reducing Deamination Bodily process in which amino groups are removed from excess proteins. This happens most often in the liver, though it also occurs in the kidneys. Hydrolysis A chemical process in which a molecule of water is added to a substance. Sulfonation An organic reaction in which a hydrogen atom on an arene is replaced by a sulfonic acid functional group in an electrophilic aromatic substitution Cytochrome P450 Enzymes located in liver or gut involved in these reactions Phase II metabolism Conjugation with an endogenous compound such as glucuronic acid, sulfuric acid, acetic acid, methyl compounds, or amino acids to form a highly polar conjugate. Role of CYP 450 enzymes and drug metabolism Phase I reaction Located in liver hemoproteins serving as the terminal oxidase multiple polymorphisms- CYP:1A2, 2A6, 2C9, 2D6, 2E1, 3A4 Carry out the bulk of hepatic metabolism Role of CYP 450 enzymes and drug metabolism Potential for drug interactions increased with 2 or more drugs metabolized via the same pathway, especially if the pathway is primary Some medications induce their own metabolism CYP:3A4 Metabolize 50% of all drugs Many different isoforms CYP:1A2-15% CYP:2C9-20% CYP:3A4-30% Factors that induce CYP metabolism Genetic variation age sex liver size liver function Factors that induce CYP metabolism Circadian rhythm Body temperature Nutritional state Exposure to drugs Exposure to chemicals Disease states that effect metabolism Liver disease Biliary disease Cardiac disease Respiratory disease Thyroid disease Disease states that effect metabolism Release of inflammatory mediators, nitrous oxide, cytokines associated with infection. Can inactivate or degrade CYP450 enzyme and reduce metabolism Ethnicities prone to slow acetylation Blacks 50% Whites 50% Asians Slow acetylation Can have profound effect on drug metabolism Multiple polymorphisms Transmitted as autosomal recessive trait Cytochrome polymorphism Defects in CYP2C19 that cause slow acetylation Interfere with mephenytoin metabolism Most common in Japanese Defects in CYP2C9 that cause slow acetylation Multiple variations of polymorphism Encode for decreased warfarin metabolism Defects in CYP3A5 that cause slow acetylation Polymorphic differences of 0% to 100% Caucasian 5% Japanese 29% Chinese 27% Koreans 30% African-Americans 73% Factors of rational drug selection Define the patient's problem Specify therapeutic objective Collaborate with patient Choose the treatment Educate patient Monitor effectiveness Process of rational drug selection Assess patient Develop working and differential diagnosis Diagnostic tests to confirm Use evidence-based guidelines Individualize for each patient Rational drug selection Novice providers use analytic, step-by-step decision making Rational drug selection Experienced providers use experience and pattern recognition. Use more systematic approach with complex patients. Schedule I drug Substances in this schedule have no currently accepted medical use in the United States, a lack of accepted safety for use under medical supervision, and a high potential for abuse. Schedule II drug Substances in this schedule have a high potential for abuse which may lead to severe psychological or physical dependence. Schedule I drug heroin, lysergic acid diethylamide (LSD), marijuana (cannabis), peyote, methaqualone, and 3,4-methylenedioxymethamphetamine ("Ecstasy"). Use in labs only Schedule II drug Narcotics-hydromorphone (Dilaudid), methadone (Dolophine), meperidine (Demerol), oxycodone (OxyContin, Percocet), and fentanyl (Sublimaze, Duragesic). Other Schedule II narcotics include: morphine, opium, and codeine. Schedule II drug Stimulants-amphetamine (Dexedrine, Adderall), methamphetamine (Desoxyn), and methylphenidate (Ritalin) and cocaine. Other substances include amobarbital, glutethimide, and pentobarbital, and secobarbital. Schedule III drugs Have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence. Schedule III drugs Narcotics- combination products containing less than 15 milligrams of hydrocodone per dosage unit (Vicodin), products containing not more than 90 milligrams of codeine per dosage unit (Tylenol with Codeine), and buprenorphine (Suboxone). Depressant-butabarbital Schedule III drugs Non-narcotic-Ketamine, Benzphetamine (Didrex), Phendimetrazine, and anabolic steroids like .Depo testosterone Schedule IV drugs Have a low potential for abuse relative to substances in Schedule III. Schedule IV drugs alprazolam (Xanax), carisoprodol (Soma), clonazepam (Klonopin), clorazepate (Tranxene), diazepam (Valium), lorazepam (Ativan), midazolam (Versed), temazepam (Restoril), and triazolam (Halcion). Benzodiazipines, meprobamate Schedule V drugs Have a low potential for abuse relative to substances listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotics. Schedule V drugs Cough preparations containing not more than 200 milligrams of codeine per 100 milliliters or per 100 grams (Robitussin AC, Phenergan with Codeine), and ezogabine. Loparimide, diphenoxylate