Principles of Pharmacology

name the basic steps in the treatment of poisoning:

(1) provide immediate cardiopulmonary support as needed (2) remove the patient from the poison or the poison from the patient (3) determine the substance causing the poisoning (4) administer any antidotes available to counteract the poison (5) continue monitoring and supporting the patient's vital organs as long as required

enzymes - give examples of drugs that bind these receptors: - carbonic anhydrase: 1 - cholinesterase: 2 - cyclooxygenase: 3 - DNA polymerase: 4 - DNA topoisomerase: 5 - human immunodeficiency virus (HIV) protease: 6 - monoamine oxidase: 7 - Na+,K+-adenosine triphosphatase: 8 - xanthine oxidase: 9

1: acetazolamide 2: donepezil and physostigmine 3: aspirin and celecoxib 4: acyclovir and zidovudine 5: ciprofloxacin 6: indinavir 7: phenelzine 8: digoxin 9: allopurinol

drug names: - a chemical name (e.g. 1) - a nonproprietary (generic) name (e.g. 2) - a proprietary name (or trade or brand name) (e.g. 3)

1: acetylsalicylic acid 2: oxacillin, ibuprofen 3: Prozac, Viagra

almost all drugs are reversibly bound to plasma proteins, primarily albumin, but also lipoproteins, glycoproteins, and β-globulins in general: - acidic drugs bind to 1, and - basic drugs bind to 2

1: albumin 2: glycoproteins and β-globulins

other macromolecules - give examples of drugs that bind these receptors: - membrane lipids: 1 - nucleic acids: 2

1: alcohol and amphotericin B 2: cyclophosphamide and doxorubicin

the rate at which a drug is distributed to various organs after a drug dose is administered depends largely on the proportion of 1 received by the organs

1: cardiac output

reductive reactions - give example of drugs: - nitro reduction: 1 - reductive hydrolysis: 2

1: chloramphenicol 2: nitroglycerin

membrane transport proteins - give examples of drugs that bind these receptors: - ligand-gated ion channels: 1 - voltage-gated ion channels: 2 - ion transporters: 3 - neurotransmitter transporters: 4

1: diazepam and ondansetron 2: lidocaine and verapamil 3: furosemide and hydrochlorothiazide 4: fluoxetine and cocaine

hormone and neurotransmitter receptors - give examples of drugs that bind these receptors: - adrenoceptors: 1 - histamine receptors: 2 - 5-hydroxytryptamine (serotonin) receptors: 3 - insulin receptors: 4 - muscarinic receptors: 5 - opioid receptors: 6 - steroid receptors: 7

1: epinephrine and propranolol 2: cimetidine and diphenhydramine 3: lysergic acid diethylamide (LSD) and sumatriptan 4: insulin 5: atropine and bethanechol 6: morphine and naltrexone 7: cortisol and tamoxifen

conjugation reactions - give example of drugs: - acetylation: 1 - glucuronidation: 2 - sulfation: 3

1: hydralazine, isoniazid 2: morphine, oxazepam 3: acetaminophen, minoxidil

oxidative reactions - give example of drugs: - aliphatic hydroxylation: 1 - aromatic hydroxylation: 2 - N-dealkylation: 3 - O-dealkylation: 4 - deamination: 5 - N-oxidation: 6 - S-oxidation: 7

1: ibuprofen, pentobarbital, and tolbutamide 2: phenobarbital, phenytoin, and propranolol 3: codeine, imipramine, and theophylline 4: codeine, dextromethorphan, and indomethacin 5: amphetamine and diazepam 6: chlorpheniramine 7: chlorpromazine and cimetidine

drug hypersensitive reactions: - type 1 reactions are immediate hypersensitivity reactions that are mediated by 1. Examples: 2 - type 2 reactions are cytolytic reactions that involve immune complement and are mediated by 3. Examples: 4 - type 3 reactions are mediated by 5. Examples: 6 - type 4 reactions are delayed hypersensitivity reactions that are mediated by 7. Examples: 8

1: immunoglobulin E antibodies 2: angioedema, urticaria ("hives"), dermatitis, and anaphylactic shock 3: immunoglobulins G and M 4: hemolytic anemia, thrombocytopenia, and drug-induced lupus erythematosus 5: immune complexes 6: inflammation, lymphadenopathy, fever (serum sickness), and Stevens-Johnson syndrome (a life-threatening form of drug-induced vasculitis) 7: sensitized lymphocytes 8: the ampicillin-induced skin rash that occurs in patients with viral mononucleosis

pharmaceutical preparations: - tablets and capsules: 1 - solutions and suspensions - skin patches - aerosols - ointments, creams, lotions, and suppositories

1: ingredients: - fillers (specific components that provide bulk) - lubricants (prevent sticking to the punch and die during manufacture) - adhesives (maintain tablet stability in the bottle) - disintegrants (facilitate solubilization of the tablet when it reaches gastrointestinal fluids)

hydrolytic reactions - give example of drugs: - amide hydrolysis: 1 - ester hydrolysis: 2

1: lidocaine and procainamide 2: aspirin, esmolol, and procaine

phases of drug biotransformation: - phase 1 biotransformation includes: 1 - phase 2 biotransformation include: 2

1: oxidative, hydrolytic, and reductive reactions 2: conjugation reactions (with an endogenous substance such as acetate, glucuronate, sulfate, or glycine)

most drugs are absorbed by 1 across a biologic barrier and into the circulation. The rate of absorption is proportional to the drug concentration gradient across the barrier and the surface area available for absorption at that site, known as 2. Drugs can be absorbed passively through cells either by lipid diffusion or by aqueous diffusion a few drugs are absorbed by 3 or by 4

1: passive diffusion 2: Fick's law 3: active transport 4: facilitated diffusion

nuclear receptors: - type 1 nuclear receptors include targets for 1 - type 2 nuclear receptors include receptors for 2

1: sex hormones (androgen, estrogen, and progesterone receptors), glucocorticoid receptors, and mineralocorticoid receptors 2: nonsteroid ligands including thyroid hormone, vitamin A and D receptors, and retinoid receptors

what is the largest family of receptors for pharmaceutical agents?

G protein-coupled receptors (GPCRs)

steps in the process of drug development in the United States:

IND: investigational new drug NDA: new drug application

what is a xenobiotic?

a xenobiotic is a drug produced outside the body, either synthetic or natural

pharmacology is divided into 2 main subdivisions:

pharmacokinetics: - the processes that determine the concentration of drugs in body fluids (e.g. plasma) and tissues over time - including absorption, distribution, metabolism (also called biotransformation), and excretion (ADME). Elimination = metabolism + excretion pharmacodynamics: - the study of the actions of drugs on target receptors and tissues - including receptor binding, signal transduction, pharmacological effects, dose-response

definition of pharmacology:

pharmacology is the biomedical science concerned with the interaction of chemical substances with living cells, tissues, and organisms

define pharmacotherapeutics:

pharmacotherapeutics is the medical science concerned with the use of drugs in the treatment of disease

define pharmacy:

pharmacy is the science and profession concerned with the preparation, storage, dispensing, and proper use of drug products

membrane-bound enzymes that serve as receptors for various endogenous substances and drugs are classified into 5 types. Name them:

receptor guanylate cyclase receptor tyrosine kinase tyrosine kinase-associated receptor receptor tyrosine phosphatase receptor serine/threonine kinase

the goal of pharmacology:

the goal of pharmacology is to understand the mechanisms by which drugs interact with biologic systems to enable the rational use of effective agents in the diagnosis and treatment of disease

define toxicology:

toxicology is the study of poisons and organ toxicity. It focuses on the harmful effects of drugs and other chemicals and on the mechanisms by which these agents produce pathologic changes, disease, and death

drug excretion - give examples of routes of excretion from the body:

urine, bile, sweat, saliva, tears, feces, breast milk, and exhaled air