For a drug to produce an effect it must overcome an individual's - ANSWER Homeostasis: physio processes meant to maintain internal cell environment
What is a graded drug response? Examples? - ANSWER Biological effects
...
For a drug to produce an effect it must overcome an individual's - ANSWER Homeostasis: physio processes meant to maintain internal cell environment
What is a graded drug response? Examples? - ANSWER Biological effects that can be measured (blood pressure, HR, diuresis, pain, coma, brochodilation)
What is a quantal drug response? Examples? - ANSWER Effects that may or may not occur, not necessarily measured (pregnancy, seizures, rash, sleep, death)
_______ is the expression of how much drug is needed to produce a biological response - ANSWER Potency
50mg drug that produces same response as 250mg drug is more potent
________ is the ability of a drug to produce a maximum effect at any dosage - ANSWER Efficacy
Morphine is more efficient at treating severe pain than Motrin. Expresses the maximum effect a drug is able to produce
___________ is the ability of a drug to produce a large response once it has occupied specific receptors - ANSWER Intrinsic activity
Does number of receptors occupied make difference in drug response?
Describe the ratio of selectivity - ANSWER Dose or concentration producing undesired effect / dose or concentration producing desired effect
Ex: A med requires 1 tab to cause desired effect with no undesired effects. When 5 tabs are taken, undesired effects present. This drug has a selectivity ratio of 5
According to the FDA Orange Book, AB rated drugs are _____________ - ANSWER Generic drugs that are considered similar enough to substitute brand names
How do brand and generic drugs differ? - ANSWER Both contain same active ingredient. Different inactive ingredients (coloring, filler) that cause differences in absorption time
__________ are large molecules, usually proteins, that interact with and mediate the action of drugs - ANSWER Receptors
Why are receptors important? - ANSWER Determine dose/effect relationship
Determine drug selectivity
Determine actions of antagonists
Framework/predictor of drug actions related to dose
_________ is the correlation of chemical structure with pharmacological activity - ANSWER Structure-activity relationship (SAR)
____ are drugs that produce receptor stimulation and conformational change every time they bind - ANSWER Agonists, or full agonists
_______ are drugs that bind to receptors but do not stimulate them - ANSWER Antagonists
________ are drugs that bind to receptors but stimulate only some of them - ANSWER Partial agonists
The ____ of G-proteins recognizes and binds to drugs - ANSWER Binding site
The __________ of G-proteins control what happens after the drug is bound - ANSWER Intracellular proteins
Activation of receptors produce intracellular changes in the binding of the G-protein receptor to other proteins that control response through molecules called __________ - ANSWER Second messengers
What enzyme so statin drugs inhibit? - ANSWER HMG-Co-A
Controls cholesterol synthesis
Define pharmacokinetics - ANSWER What the body does to a drug
Absorption, distribution, metabolism, excretion
How are oral meds absorbed? - ANSWER Stomach > small and large intestines > pass through intestinal lining > possibly metabolized in liver > bloodstream
How do enteric-coated meds work? - ANSWER Protect medication in the stomach and only disintegrate in the gentler intestine. Keeps meds from being absorbed too rapidly by stomach
How do sustained-release meds work? - ANSWER Allow slow dissolve in intestines
How are ocular medications made to avoid sensitivity/discomfort? - ANSWER Buffered and isotonic
Define bioavailability - ANSWER - The fraction of unchanged drug that reaches the systemic circulation.
- The amount of free drug that binds to target site and produces effect.
Molecules with molecular weight less than _______ are best for passive diffusion - ANSWER 500
The presence of some plasma proteins in the blood reflects ___________ function - ANSWER Liver
Many are made in liver, such as Albumin
How do plasma proteins affect drug distribution? - ANSWER Bind to drugs and circulate through bloodstream, not diffusion. Protects drug from metabolism in liver and excretion in kidneys, so drug time can be extended in body
Describe the relationship of Warfarin and plasma proteins - ANSWER Warfarin binds to PP, and bound areas cannot interact with receptors. Warfarin is 98% bound proteins and 2% circulating. The 2% produces an effect.
__________ involves the chemical alteration by enzymes into new molecules - ANSWER Metabolism, new molecules called metabolites
______ is the process of changing one chemical into another, which either produces or uses energy - ANSWER Metabolism
Why is the liver a major site for metabolism? - ANSWER Contains high amounts of enzymes and is first organ drugs encounter once they are absorbed by the GI tract
What is P450 CYP? - ANSWER Family of enzymes that metabolizes drugs
___________ involves oxygenation, reduction, and hydrolysis reactions, which prepare drug molecules for further metabolism - ANSWER Phase 1 of metabolism, or "non-synthetic reaction"
______ involves drug molecules being metabolized and something is added to the drug to synthesize a new compound - ANSWER Phase 2 of metabolism, or "synthetic or conjugation reaction"
CYP3As are a major subfamily of enzymes expressed in the human liver in 3 forms: - ANSWER CYP3A4
CYP3A5
CYP3A7
What does CYP3A7 do? - ANSWER Present in fetus and DC's after birth
What does CYP3A4 do? - ANSWER Major drug-metabolizing enzyme
Azole antifungals, statin drugs, corticosteroids (prednisone, prednisolone, dexamethasone), anticonvulsant (carbamazepine)
What does CYP3A5 do? - ANSWER Metabolizes same drugs as 4, but not as well
______ are inactive compounds that rely on metabolism to activate - ANSWER Prodrugs
Example: L-DOPA (Parkinson's) can pass into brain, enter cells, and be converted to Dopamine
Describe relationship of grapefruit juice on drugs - ANSWER Grapefruit juice inhibits CYP3A4, and can increase blood levels of drugs up to a day before administration
Older statin drugs
Approx _____ of blood flows through the kidneys per minute. What is this called? - ANSWER 125 ml/ min
Glomerular filtration rate (GFR)
Urine can be made acidic with what fluid? - ANSWER Ammonium chloride
Urine can be made basic by what fluid? - ANSWER Sodium bicarb
Excretion: The liver secretes about ______ of bile daily - ANSWER 1 liter
Name examples of excretion by the lungs - ANSWER Anesthetic gases, like nitrous oxide
Alcohol consumption: ethanol excreted with each exhale (breathalyzer)
Ketones: poorly controlled diabetics have fruity breath
_________ refers to the time between administration and first sign of drug effect - ANSWER Onset of action
_______ refers to the point at which amount of drug being absorbed and distributed is equal to amount being metabolized and excreted (max concentration of drug) - ANSWER Peak of action
________ is the continued entry of a drug into the body with levels above minimum effective concentration - ANSWER Duration of action
What is the minimum effective concentration? - ANSWER Level below which therapeutic effects will not occur
What is the minimum toxic concentration? - ANSWER Level above which toxic effects begin
What is the therapeutic index? - ANSWER Minimum toxic concentration- minimum effective concentration
_________ is the percentage of a drug that is absorbed and available to reach tissues - ANSWER Bioavailability
It takes _________ lives to get to a steady state blood level, and it takes _________ lives to totally eliminate drug from the body - ANSWER 4-5.5
Describe relationship of distribution and blood supply - ANSWER Drugs travel to areas of high blood supply first
Protein binding
Free drug + Bound drug = ? - ANSWER Drug-protein complex
Describe relationship of amount of plasma proteins with drug distribution - ANSWER Low plasma proteins >> more free drug in circulation
Low plasma proteins leads to higher amounts of free drug. What can this cause? - ANSWER Toxicity
More drug eliminated
__________ drugs deposit in bone and teeth - ANSWER Tetracyclines
Only ___________ drugs can cross blood-brain barrier - ANSWER Lipid-soluble
Which variations can occur in isoenzymes, like CYP 450 enzymes? - ANSWER Developmental and genetic differences.
Some disease processes can alter enzymes (i.e. CF alters CYP2D9)
For drug to be filtered by glomeruli, it must ...? - ANSWER Be unbound from protein (free)
Water-soluble
_________ involves filtrate moving through nephron, molecules reabsorbed into blood - ANSWER Passive glomerular filtration
________ involves the movement of ions, amino acids, and glucose back into circulation back into cells and into the plasma - ANSWER Tubular reabsorption
Describe differences in gamete versus sperm cell production in males/females - ANSWER Women are born with all their gametes. Men start producing sperm at puberty and continue into testosterone wanes (60s, 70s)
Gastric emptying time is ______ in females. Why? What does this affect? - ANSWER Slower, likely r/t estrogen
Drugs absorbed in stomach will stay longer
Describe volume of distribution of lipophilic drugs in females - ANSWER Females have more fat. Absorbed quickly and stay longer
Women have ____ rates of metabolism for CYP450 3A4 substrates - ANSWER Higher, clear drugs faster
Describe opiates and women - ANSWER Greater analgesic effect but more adverse reactions (n/v)
Women age 15-50 have __ QT intervals, making them prone to arrhythmias - ANSWER longer
Describe Warfarin and Asprin in women - ANSWER Warfarin: less benefits with higher mortality r/t bleeding
Aspirin: Lowers risk for stroke but not MI
Describe woman and antipsychotic drugs - ANSWER Most effective in women but more adverse reactions
Why do women experience adverse reactions with antipsychotic drugs? - ANSWER R/t anti-dopaminergic actions of estrogen. Should prescribe lower doses for women
Antipsychotics: women respond better to __________ class, men to ________ class - ANSWER Women: SSRIs
Men: Tricyclic antidepressants
Describe antiretroviral drugs and women - ANSWER More severe adverse reactions, allergic reactions, etc.
What makes up the female athlete triad? - ANSWER Amenorrhea
Osteoporosis
Disordered eating
Describe physiologic of female athlete triad - ANSWER Poor eating/overexercise suppresses hypothalamic-pituitary-ovarian axis >> cause reduced estrogen, amenorrhea, osteoporosis
______ is absence of menses for 6 months in a girl who has had a period - ANSWER Secondary amenorrhea
________ is absence of menses by age 13 or 15 with secondary sex characteristics - ANSWER Primary amenorrhea
What are strategies to reduce osteoporosis in adolescent females? - ANSWER Increase daily calcium to 1300 mg and vitamin D to 400
How can menses be resumed in adolescents? - ANSWER Decrease exercise, increase PO intake, increase BMI
Describe bone formation pattern in women - ANSWER 40% bone in adolescence, continues to age 30, then bone loss starts
Long-term Depo-Provera (injectable birth control) has been linked to - ANSWER Significant bone density loss
Due to loss in bone density, Depo-Provera should not be used for longer than _______ - ANSWER 2 years
In pregnancy, drug absorption from which sites increase? - ANSWER Lungs and skin
Cardiac output in pregnancy may be _______% higher than prepregnancy - ANSWER 30-50% higher
Drug clearance ____ in pregnancy - ANSWER Increases
Why is iron deficiency anemia common in pregnancy? - ANSWER Expansion of plasma volume without expansion of hemoglobin mass
What can iron deficiency anemia lead to in pregnancy? - ANSWER Infection, fatigue, pre-eclampsia, post-part hemorrhage
Daily iron intake of ____ is needed during pregnancy - ANSWER 30 mg, start at first visit
Oral iron should be taken with ______ to increase absorption - ANSWER Vitamin C, after meals to reduce GI irritation
Pregnant women should limit daily caffeine to _____ - ANSWER 150-300 mg
How do carbon monoxide and nicotine (in smoking) affect pregnancy? - ANSWER CM: competes for O2 sites on fetal hgb
N: causes materal/fetal vasoconstriction
Alcohol causes decreased absorption of ____ and _______ - ANSWER Folic acid, thiamine
Acceptable herbal remedies in pregnancy include... - ANSWER Ginger (n/v)
Horse chestnut (vericose veins)
Meadowsweet (heartburn)
Estrogen-like properties can be found in what foods/herb? - ANSWER Ginseng, black cohosh, licorice
Carrots, yams, soy
For menopausal women, nutrition supplements should contain which vitamins/minerals? - ANSWER E, D, B
Calcium
What amount of exercise is recc for menopausal women? - ANSWER 30 min moderate 6 days/week
Life expectancy of white women? - ANSWER 80.5 years
What is the mean age of menopause? - ANSWER 51.3 years
It is recc that HRT of estrogen and progesterone in menopausal women with a uterus be no longer than ________. Why? - ANSWER 3-5 years
Risk of breast cancer
_______ therapy alone can be safe long-term in menopausal women with a uterus - ANSWER Estrogen
Define dysmenorrhea - ANSWER Pain before or during menstruation
What causes primary dysmenorrhea? - ANSWER Increase myometrial activity with contractions induced by prostaglandings in second half of menstrual cycle
What is med treatment for dysmenorrhea? - ANSWER First-line are NSAIDS taken 2-3 days before menses
Oral contraceptives
What are complementary meds used to treat dysmenorrhea? - ANSWER Thiamine (b12), magnesium, vitamin E, omega 3
What causes secondary dysmenorrhea? - ANSWER Endometriosis, adenomyosis, PID, polyps, fibroids
Effective treatment options for PMS? - ANSWER Aerobic exercise
Reduce caffeine
Reduce salt
Ibuprofen 500-1000 mg/day in days 17-28 of cycle
Reduce sugar, chocolate, red meat, dairy, alcohol
Take calcium supp
How is premenstrual dysphoric disorder diagnosed? - ANSWER Must have 5 or more symptoms, including 1 "core" symptom
-Depressed mood
-Anxiety
-Liability
-Anger
-Lack of interest
-Fatigue
-Sleep issues
-Cravings/app changes
Describe symptom timing in premenstrual dysphoric disorder - ANSWER Cyclical, go away when menses starts
_______ are first-line therapy for premenstrual dysphoric disorder - ANSWER SSRIs (fluozetine, paroxetine, sertraline
Also, prostaglandins, NSAIDs, birth control
Calcium supp of ____________ mg/day reduce PMS symptoms - ANSWER 1200-1600mg/day
_____ are second-line drugs for PMDD - ANSWER Tricyclic clomipramine and benzodiazepine
Define endometriosis - ANSWER Presence of functioning endometrial tissue outside uterus. Inflammation leads to pain. Can cause fibrosis, scarring, infertility
Describe drug therapy for endometriosis - ANSWER GnRH for 3 months or Danazol for 6 months
NSAIDs for pain
Birth control
It is recommended that those with endometriosis limit xenestrogen exposure. Which foods contain this? - ANSWER Dairy, beef, chicken
Which supplements may help endometriosis inflammation? - ANSWER Calcium, magnesium, omega-3
Which drug is recommended to reduce HIV trans from mother to baby in pregnancy? - ANSWER Zidovudine, triple combined antiretroviral
How is infertility defined? - ANSWER Inability to conceive after trying for 1 year
Women over 35 should seek fertility eval if unable to conceive after ______ - ANSWER 6-9 months
What does polycystic ovarian syndrome do? - ANSWER Endocrine imbalance. High levels of estrogen, testosterone, LH
Low FSH
Impaired glucose tolerance>> risk of DM2
Ovaries double in size with cysts
What med could be used to treat symptom of hirsutism in polycystic ovarian syndrome? - ANSWER Oral contraceptives
In PCOS, the prescription of _______ and _______ can manage DM2, lower testosterone, reduce acne, hirsutism, obesity, etc - ANSWER Insulin and metformin
At what age should mammograms start? - ANSWER 40
At what age should colonoscopy be done? - ANSWER Over 50
Bone mineral density testing is recommended for women over _____ - ANSWER 65
What are the leading causes of death in men? - ANSWER Heart disease, cancer, accidents
_______is failure of the testes to produce androgen, sperm, or both - ANSWER
[Show More]