click below
click below
Normal Size Small Size show me how
Pharmacological Prin
week 2 pharm
Question | Answer |
---|---|
Pharmacokinetics | what the body does to a drug- the study of the movement of drugs in the body- processes of absorption, distribution, metabolism and elimination |
Pharmacodynamics | study of how a specific drug affects the body- the relationship between the dose and response, i.e., the drug's effects- depends on the drug binding to its target. |
Pharmacotherapeutics | The study of the therapeutic uses and effects of drugs in patients |
Pharmacognosy | the study of medicinal drugs derived from plants or other natural sources. |
Pharmacogenetics | The branch of pharmacology concerned with the effect of genetic factors on reactions to drugs- therapeutic effect as well as adverse effects |
Pharmacokinetics/Absorption | method and rate at which drugs leave site of administration – Note oral to small intestines to liver |
Distribution | occurs when drug leaves the systemic circulation and enters the cells. Note that fat and protein content affect distribution. ***lipophilic vs. lipophobic***. So, Hydrophobic (lipophilic) and hydrophilic (lipophobic) |
MOST PSYCHOTROPIC MEDICATIONS ARE | LIPOPHILIC AND HIGHLY PROTEIN-BOUND= What does this entail? – less protein, more active drug in circulation, more toxicity. Low albumin levels as in malnourished, old, cachexic patients may experience more toxicity. |
Metabolism | process by which the drug becomes chemically altered in the body |
First-pass Metabolismpr | process by which the drug is metabolized by CYP450 enzymes in the intestines and liver prior to going into the systemic circulation. |
Elimination | process by which the drug is removed from the body |
HALF-LIFE(T1/2) | time needed to clear 50% of the drug from plasma. A very important consideration for drug dosing. |
STEADY STATE | point at which the amount of drug eliminated between doses is approximately equal to the dose administered. It takes approximately five half-lives to achieve a steady state and five half-lives to completely eliminate a drug. |
Approximately 10% of Caucasians are poor metabolizers of the | P450 2D6 enzyme |
Approximately 20% of Asians may have reduced activity of the | P450 2C19 enzyme |
First –pass metabolism activity of P450 enzyme | 2C9, 2C19, 2D6 and 3A4 may give rise to underexposure of certain drugs in adolescents and adult. |
1A2 enzyme pathway on the other hand, is delayed possibly leading to | toxicity of drugs that are substrates of this pathway – like some antipsychotic medications |
Enzyme Inducers can | decrease serum level of other drugs that are substrates of that enzyme causing sub therapeutic drug levels |
Enzyme inhibitors on the other hand can | increase serum levels of drugs that are substrates of that enzyme causing toxic drug levels. |
Liver disease – affects first-pass metabolism and can cause | drug toxicity |
Kidney disease – can affect drug clearance For example, can reduce renal clearance of | NSAIDs, may increase serum level of drugs excreted by the kidneys (e.g., lithium) |
Target sites | receptors, ion channels, enzymes, carrier proteins |
Agonist effect | binds to receptor and activates a biological response |
Inverse agonist effect | causes opposite effect; binds to different area on receptor compared to full agonist. |
Partial agonist effect | drug does not fully activate the receptors |
Antagonist effect | binding to the receptor does not activate a biological response |
Ion channels | sodium, potassium, calcium, chloride can be open or closed at certain times |
Neurotransmitters | may be excitatory or inhibitory depending on the ion channel they gate. |
excitatory response | Depolarization(opening of sodium and calcium channels so these go into the cells). Inhibitory response |
Enzymes | e.g monoamine oxidase inhibitors(MAOIs) inhibit action of a particular enzyme thus increasing the neurotransmitter available |
“Another site for drug actions is carrier proteins or reuptake pumps, which transport neurotransmitters out of the synapse and back into the presynaptic neuron to be recycled or reused | Some drugs, such as selective serotonin reuptake inhibitors (SSRIs), will inhibit reuptake pumps, thus increasing the synaptic availability of the neurotransmitter” |
Potency | relative dose needed to achieve certain/desired effects |
Therapeutic Index | measure of toxicity or safety(ratio of the median toxic dose to the median effective dose) |
high therapeutic index | (therapeutic dose and toxic dose are far apart). Example divalproex 50-125mcg/ml***aim at 50-100mcg/ml |
- low therapeutic index | (therapeutic dose and toxic dose are close together). Example lithium 0.5-1.2mEQ/L |
Tolerance | becoming less responsive to a particular drug over time |
Tachyphylaxis | “an acute decrease in the therapeutic response” |
Benzodiazepines Teratogenic risk | floppy baby syndrome, cleft palate |
Carbamazepine Teratogenic risk | neural tube defect |
Divalproex sodium Teratogenic risk | neural tube defects, specifically spina bifid, atrial septal defect, and possibly long-term developmental defects. |
Lithium Teratogenic risk | Congenital heart defect (Ebstein’s anamoly) |
“Ebstein anomaly is a | congenital malformation of the heart -apical displacement of the septal and posterior tricuspid valve leaflets, leading to atrialization of the right ventricle with a variable degree of malformation and displacement of the anterior leaflet” |
Medications that induce mania | Steroids, Disulfiram(Antabuse), Isoniazid(INH), Antidepressants in persons with bipolar disorder |
Medications that can cause false positive drug screens | (Valium)alcohol, (Sertraline)benzodiazepines, (antibiotics, NSAIDs)cocaine, (Quinolones, rifampin, poppy )opioids, (cough syrup, Dextromethorphan)methadone/PCP, (Adderall, bupropion, fluoxetine, trazodone, ranitidine, decongestants, Serzone) amphetamines |
NPs are licensed by the Drug Enforcement Administration(DEA) to prescribe schedule | II-V(some restrictions within the schedules may apply, especially according to individual States. |
Schedule I drugs, substances, or chemicals are defined as drugs with | no currently accepted medical use and a high potential for abuse. heroin, lysergic acid diethylamide (LSD), marijuana, 3,4-methylenedioxymethamphetamine (ecstasy), methaqualone, and peyote |
Schedule II drugs, substances, or chemicals are defined as drugs with | a high potential for abuse, with use potentially leading to severe psychological or physical dependence. These drugs are also considered dangerous. |
Schedule 2 drugs | Combination products with less than 15 milligrams of hydrocodone per dosage unit (Vicodin), methamphetamine, methadone, hydromorphone (Dilaudid), meperidine (Demerol), oxycodone (OxyContin), fentanyl, Dexedrine, Adderall, and Ritalin |
Schedule III drugs, substances, or chemicals are defined as drugs with a | moderate to low potential for physical and psychological dependence. |
Schedule III examples | Products containing less than 90 milligrams of codeine per dosage unit (Tylenol with codeine), ketamine, anabolic steroids, testosterone |
Schedule IV drugs, substances, or chemicals are defined as drugs with | a low potential for abuse and low risk of dependence. Xanax, Soma, Darvon, Darvocet, Valium, Ativan, Talwin, Ambien, Tramadol |
Schedule V drugs, substances, or chemicals are defined as drugs with | lower potential for abuse than Schedule IV and consist of preparations containing limited quantities of certain narcotics. |
Schedule V drugs are generally used for | antidiarrheal, antitussive, and analgesic purposes. cough preparations with less than 200 milligrams of codeine or per 100 milliliters (Robitussin AC), Lomotil, Motofen, Lyrica, Parepectolin |
Cognitive Behavioral Therapy (CBT) | for residual psychotic symptoms and anxiety disorders |
Dialectical Behavioral Therapy (DBT) | teaches distress tolerance skills to people with personality disorders, chronically suicidal patients |
Motivational Interviewing | for health behavior change including smoking, weight loss, alcohol use, exercise |
Behavioral Activation | great for patients that are “stuck” |