Endocrine Pharm Flashcards

Question

Danazol

Answer 1

Anti-progestin - Weak progestin, androgen and glucocorticoid → - --suppresses ovarian function -treat Endometriosis** Adverse: -hirsutism, deepening voice, acne, oily skin Contra: - liver dysfunction - pregnancy or breastfeeding

Answer 2

-combo of estrogen & spironolactone derivative --mineralcorticoid antagonist - ↓ water retention → reduces PMDD symptoms - very low androgenic properties - Inhibit ovulation → no LH surge - ↓ implantation → change cervical mucosa & endometrium - discontinuation → withdrawal bleeding at end of cycle - ↓ endometrial & ovarian cancer - ↓ acne - ↓ PCOS ADVERSE: estrogen → weight gain, nausea, edema Progestin → weight gain & depression ***-thromboembolic & clotting disorders***** --↑ synthesis of coagulation factors & fibrinogen --↑ risk of thromboembolic and clotting disorders --↑ risk if >35 and smoke -mild HTN -Migraine (may be warning of stroke) -Teratogenic - 1st trimester -↓ Fertility → gonadotropin for 3 months after stopping -Breast feeding ABSOLUTE CI: - *Thromboembolic phenomena - *estrogen dependent neoplasms - thrombophlebitis - cerebrovascular disorders - pregnancy

Answer 3

Androgen Virilizing (Androgenic) effects: - spermatogenesis - sexual development Anabolic effects: - ↑ bone density - *↑ AA incorporation into muscle - ↑ RBC mass - antagonize catabolic effects of glucocorticoids MEN → testicular deficiency -avoid use for impotence in aging → ↑ risk prostate cancer FEMALES → hypopituitarism (estrogen & androgens -BOTH → protein loss ``` Adverse effects: MEN: -Inhibits release of LH and FSH --↓ testosterone production --↓ spermatogenesis WOMEN: -masculinization- deep voice, clitoral enlargement -loss of gonadotropins (atrophy of breast & uterus) -pregnant → pseudo-hermaphroditism BOTH -oily skin, acne -↓ HDL -psychological changes→ aggression, depression, psychosis ``` CI -children → closes epiphyseal plate

Answer 4

Androgen synthesis inhibitor -antifungal → need 4x anti fungal dose - inhibits 17α hydroxylase → ↓ androgens then ↓ cortisol - -higher dose inhibit cholesterol → pregnenolone (all steroids) Women: -hirsutism, premenstrual syndrome, cystic acne Men - prostate tumors - SE of gynecomastia, ↓ libido, impotence - HIGH DOSES in Cushing's before surgery or radiation - -**most effective inhibitor of steroid synthesis in pts w/ Cushings DISEASE (problem at pituitary; ↑ ACTH)

Answer 5

Androgen synthesis inhibitor & Anti-androgen - mineralcorticoid antagonist - -competes w/ aldosterone for binding at low doses - -competes for androgen & estrogen receptors at *↑ doses - reduces 17α-OH activity→ ↓ glucocorticoids & androgens Use: - *hirsutism & PMS - *precocious puberty (both sexes) - HTN - primary aldosteronism - *ascites w/ cirrhosis Adverse: - hyperkalemia - gynecomastia & impotence → men - menstrual irregularites → women

Answer 6

Anti-androgen -↓ male accessory sex organ function Use: - prostate cancer w/ **Leuprolide (GnRH agonist) - topically → male pattern baldness, hirsutism Adverse: - mild hepatotoxic - Bicalutamide is less hepatotoxic - -1x day dosing - affects libido

Answer 7

5α-reductase inhibitors - ↓ DHT - ↑ testosterone - ↑ TSH - ↓ total serum PSA - supress male sex accessory organ (prostate) w/o affecting libido Use: - BPH - male pattern baldness Adverse: - impotence (ejaculation dysfunction too) - ↓ libido CI: - pregnancy → teratogenic to male fetus - may mask ↑ PSA due to prostate cancer

Answer 8

ACTH → ↑ glucocorticoids & androgens - used diagnostically to distinguish b/w 1º (adrenal malfunction) and 2º (pituitary malfunction) adrenocortical insufficiency - 1º = Addisons - if ↑ in cortisol → pituitary problem - no ↑ in cortisol → adrenal malfunction

Answer 9

Mineralcorticoid--zona glomerulosa (when and why) - has both mineralcorticoid & glucocorticoid activity - -high glucocorticoid - -much more significant mineralcorticoid properties - -(10 : 250) - effects similar to aldosterone - -↑ Na and H2O retention - -↑ K and H loss -use: salt-losing adrenogenital syndrome --given w/ cortisone for replacement therapy in --→ 1º adrenal insufficiency (problem w/ adrenal) 2º adrenal insufficiency → just cortisone

Answer 10

Mineralcorticoid synthesis inhibitor (tx cushing syndrome) - inhibits cholesterol → pregnenolone (opposite of ACTH) - -inhibits ALL steroid synthesis - -inhibits aromatase enzyme-- estrogen synthesis -Tx in Cushing SYNDROME (not at pituitary) --adrenal carcinoma or ectopic ACTH-tumor -Tx Metastatic Breast and Prostate cancer that has not responded to tamoxifen or anti-androgen - can cause adrenal insufficiency → give w/ corticosteroids - inhibits estrogen synthesis - less effect on testosterone

Answer 11

Adrenocorticolytic (tx cushing's DISEASE) - selective atrophy of Zona Fasciculata & Reticularis - -binds mitochondrial proteins → ↓ synthesis of corticosteroids - 1º adrenal carcinoma when surgery or rad not possible - can produce remission of Cushing's DISEASE (at pituitary) -severe GI distress

Answer 12

Glucocorticoid synthesis inhibitor - selective inhibitor of 11β-hydroxylase terminal enzyme in cortisol synthesis - -↓ cortisol levels - -↓ deoxycorticosterone → ↓ aldosterone - -↑ 11-deoxycortisol → sustains aldosterone function w/o much glucocorticoid effect - tests of adrenal function & short term management of Cushings - only drug in this class → pregnant women - hirsutism → androgen shunt

Answer 13

FAT, CHO, PROTEIN - **↑ gluconeogenesis & glycogen storage → LIVER - -catabolize protein → neg. nitrogen balance - -↑ AA in blood - -↑ activity & amount of enzymes - **↑ Lipolysis - -↑ plasma FFA - **redistribution of body fat → moon face, buffalo hump - **Antagonizes insulin → hyperglycemia & glycosuria - -↓ glucose use in muscle and fat CARDIOVASCULAR (can treat shock) - ↑ vasc. responsiveness to SNS → hypertension - ↑ cardiac output - some Na and H2O retention → edema - -↓ K+ ENDOCRINE - immediate → ↓ release of CRH → ACTH - Chronic → ↓ other endocrine systems - -GH - -LH → sex hormones → ↓ reproduction - -TSH → Thyroid - ↑ PTH → ↑ osteoclast → less Ca in bone - Inhibits action of Vit D → ↓ Ca deposition into bones - ↑ Epinephrine production in adrenal medulla - ↓ catecholamine re-uptake IMMUNE - ↓ inflammatory & immunological responses (ulcers) - -blocks all steps in inflammatory process - -inhibits PLA2, COX2, Cytokines (TNFα), IgE (histamine) - blocks early (edema, fibrin, PMN migration, phagocytosis) - blocks late (collagen synthesis & deposition) wound heal - Lympholytic effects (CLL & MM) CNS - mood elevation, insomnia, restlessness, anxiety - depression or psychosis GI -peptic ulcers → ↓ immune response to H. pylori Misc. side effects of long term use - cataracts - ↑ intraocular pressure - glaucoma - acne, skin atrophy/thinning, striae, bruising ``` CI → none for adrenocortical insufficiency -systemic bacterial infection -poorly controlled diabetes -osteoporosis peptic ulcer -heart disease or HTN w/ CHF ```

Answer 14

- EQUAL mineralcorticoid & glucocorticoid (1 : 1) - replacement therapy → adrenal insufficiency - -2º adrenal insufficiency (Addison's) - - + fludrocortisone → 1º insufficiency - Cortisone is same except: - -must be converted to hydrocortisone by liver - -has 80% anti-inflammatory & sodium retaining potency

Answer 15

Higher anti-inflammatory effects & minor salt-retaining (4 : 0.3) - Prednisone must be converted to prednisolone in liver to be active - asthma treatment

Answer 16

Highest anti-inflammatory effects & NO salt-retaining (5 : 0) -asthma treatment

Answer 17

Highest anti-inflammatory effects & NO salt-retaining (30 : 0) - Cerebral edema - -able to enter CNS -used when endogenous cortisol levels have to be measured → doesn't cross react

Answer 18

Highest anti-inflammatory effects & NO salt-retaining - most commonly prescribed glucocorticoid for: - -INHALED and INTRANASAL use

Answer 19

Uterine stimulant--DO ``` INDUCES LABOR at term → DOC --timed contractions-- on then off --augment labor --IV infusion PREVENTION of HEMORRHAGE --1st line is massage, then oxytocin? --IM route STIMULATION of MILK LET DOWN reflex --nasal application ``` ADVERSE - water intoxication → ADH like effect - uterine rupture (large dose) - anaphylaxis - sinus bradycardia of FETUS → extreme contractions - -arrhythmias, fetal death CI → any obstruction, scaring, or delivery complications

Answer 20

Uterine stimulant - activation of 5HT & α-adrenergic receptors - -→ contraction of uterine SM - used AFTER labor and delivery of placenta - -firm contractions → ↓ uterine bleeding - -2º line after *uterine massage & *oxytocin → PPH - NEVER use to induce labor → contractions too strong - -→ fetal hypoxia -Contra → Hepatic or Renal disease

Answer 21

Uterine stimulant -synthetic prostaglandin E2 - expulsion of uterine contents: intrauterine fetal, **abortion - -suppository - CERVICAL RIPENING prior to delivery at term - -gel to cervix Adverse: * ***-GI disturbances, vomiting diarrhea--can be very serious - -only administer in presence of medical personnel CI if mother or fetus have issues - for abortions if pts has: - -acute pelvic inflammation - -acute cardiac, pulm, renal, hepatic disease - -asthma, HTN, anemia, jaundice, or epilepsy

Answer 22

Uterine stimulant -derivative of PGF2α - abortion b/w 13-20th week (2nd trimester) - treat PPH if 1) massage, 2) oxytocin, 3) ergots fail Adverse: -Vomiting and Diarrhea CI for abortions if pts has: - -acute pelvic inflammation - -acute cardiac, pulm, renal, hepatic disease - -asthma, HTN, anemia, jaundice, or epilepsy

Answer 23

Tocolytic - relaxes uterine muscle probably by direct effect--unkown - used as **1st line drug depending on choice - pre-eclamptic pts → prevent convulsions - treat eclamptic pts (FDA approved) -slowly given via IV → sig. hypoTN or systole if too fast

Answer 24

Tocolytic (CCB) - blocks L-type Ca channels → ↓ uterine contraction - -starting to be 1st line tocolytic -Do not combine w/ MgSO4 → CV collapse

Answer 25

Tocolytic (NSAID) - ↓ prostaglandin synthesis → PG lead to contractions - -1st or 2nd line drug ADVERSE -partial closure of fetal ductus arteriosus

Answer 26

Tocolytic -Emergency use only → UTERINE RUPTURE only

Answer 27

Tocolytic - Direct relaxant effect on myometrium - inhibition of oxytocin release -inhibits premature labor

Answer 28

- Estrogen & tamoxifen ↑ TBG → ↓ effect - Glucocorticoids & androgens ↓ TBG → ↑ effect - Salicylates → displace thyroxine from TBG - SNS stimulants → cardiotoxicity (weight loss) - Iodides & Lithium → ↓ release or synthesis of T3/T4 - -Amiodarone contains iodide - Antacids → ↓ absorption of thyroxine - Phenytoin, carbemazepine, rifampin → ↑ metabolism - Warfarin → hyperthyroidism ↑ degradation of vit K clotting factors → ↑ warfarin response (excess bleeding Anti diabetic drugs → adjust dose for effects of T3 Corticosteroids → ↓ metabolism w/ hypo & ↑

Answer 29

Sodium salt of T4 - DOC for treating hypothyroidism - -may produce normal levels of T3 and T4 - -treat non endemic goiter, Hashimoto's, thyroid carcinoma - -Prevent goiter if taking drugs that interfere - titrated to individual - should keep TSH levels in normal range - -TSH should be measured 4-6 weeks after adjusting T4 - ↑ gradually, esp w/ → myocardial dz or atherosclerosis SE → symptoms of hyperthyroidism (looks like SNS stim) DRUG INTERACTIONS

Answer 30

Sodium salt of T3 - Used for initial therapy of Myxedema (hypothyroidism) and myxedema coma - -to achieve normal thyroid activity FASTER - NOT for maintenance therapy

Answer 31

Thioamide-- hyperthyroidism treatment - First line treatment for Graves disease - ↓ synthesis of thyroid hormone in thyroid gland - -↓ incorporation of Iodine, synthesis, prevent coupling Methimazole → more potent & longer lasting - -doesnt inhibit peripheral conversion (T4 → T3) - -can cause birth defects PTU → inhibits peripheral conversion → more rapid effect - -LIVER INJURY OR FAILURE - -should only be used if Methimazole can't be - -early pregnancy - Granulocytopenia & agranulocytosis → most serious SE - -first sign is SORE THROAT - -reverses when drug is stopped - Itching and skin rash - Goiter due to ↑ TSH

Answer 32

Hyperthyroidism treatment - Excess Idodide → ↓ synthesis of T3 & T4 - -rapid ↓ in release of thyroid hormone - ↓ vascularity & thyroid content → before thyroid surgery - Prevents RADIOACTIVE iodine uptake -not good solo treatment → wears of 2-8 weeks (thyrotoxicosis)

Answer 33

Hyperthyroidism treatment -enters thyroid and gets trapped → β rays destroy tissue - Hyperthyroidism in **elderly and **heart disease - -low dose → diagnostic procedure - -high dose → thyroid ablation -causes hypothyroidism

Answer 34

β-blocker--Hyperthyroidism treatment - ↓ S/S: tremor, tachycardia, anxiety, heat intolerance, sweat * *-↓ peripheral conversion of T4 to T3 by liver - -↓ potency of circulating thyroid hormone (specific to propranolol) -used to prepare for surgery and waiting for other drugs to take effect - CI in *asthma or *obstructive airway disease - caution w/ diabetes - VERAPAMIL if propranolol is CI

Answer 35

- binds to nuclear receptor → gene regulation - stimulate osteoclast → RANKL - ↑ intestinal Ca+ absorption (↑ phosphate too) - ↓ renal Ca+ excretion (↓ excretion of phosphate too) - ↑ bone resorption - stimulate collagen synthesis in osteoblasts - TX: osteomalacia, rickets, hypophosphatemia, hypoPTH - ensure optimal Ca utilization CAUTION w/ Sarcoidosis & Kidney stones

Answer 36

- ↓ PTH secretion - ALONE → can't prevent or treat osteoporosis - -needed for other treatment to work - different rates of dissolution → varied absorption - take throughout day (at least 2x) - inhibits Iron absorption - inhibits absorption of thyroid medication CAUTION w/ Sarcoidosis & Kidney stones

Answer 37

- ↓ bone resorption of Ca+ & phosphate - -w/ time BOTH resorption & formation ↓ - antagonizes actions of PTH - Prevent vertebral compression fractures (not other types) - reduces back pain before change is seen - INTRANASALLY or IV → destroyed in GI - -allergic reactions - -rhinitis & sinusitis - -nausea & vomiting after INJECTION only

Answer 38

Recombinant PTH - MXN not fully understood--stimulates osteoblast & -clast - -**intermittent spikes → ↑ formation > ↑ resorption -Treat osteoporosis, ↓ fractures - -**ONLY ANABOLIC osteoporosis therapy - useful in pts w/ severely low bone mass - -anabolic action ↓ w/ time - treat hypoparathyroidism -Hypercalcemia & Hypercalceiuria may occur CI: OSTEOSARCOMA (caution if susceptible)

Answer 39

RANKL antibody - inhibits RANKL → osteoclasts can't mature - -↓ bone resorption - osteoporosis treatment in postmenopausal women w/ history of fractures - ↑ bone mass and strength in cortical & trabecular bone -1 injection/ 6 months ADVERSE: hypocalcemia, cellulits, eczema - suppresses bone FORMATION - osteonecrosis of jaw w/ metastatic cancer CI ABSOLUTE: Hypocalcemia & pregnancy

Answer 40

Bisphosphonates - Inhibit osteoclast activity and bone resorption - replaces phosphate in Ca salt → blocks hydroxyapatite - -strengthen bone, ↑ density - -inhibit osteoclast resorption -First line treatment for osteoporosis & paget's disease - oral absorption is very poor - -take 2 hours before breakfast w/o Ca or Mg - -4oz water to flush into stomach - -remain upright 30-60 → ↓ GI irritation IV- administer slowly → RENAL toxicity ORAL adverse: abdominal pain, upper GI irritation, esophageal ulceration, constipation, diarrhea, flatulence --not for pts w/ esophageal disease or can't stand for 1 hr ALL: nausea, vomiting, --osteonecrosis of Jaw after major dental work

Answer 41

Calcium receptor agonist - binds to calcium sensing receptor; esp. at parathyroid - Blocks PTH release - treat 2º hyperparathyroidism - -chronic kidney disease & Parathyroid carcinoma

Answer 42

Short Acting β2 agonist (DoA 4-6 hours) - fast acting → stop asthma attack in progress - SM relaxation & stabilize mast cells - DoA: 4-8 hours SE: Tachycardia, nervousness & dizziness, tremor - -short lived - -tolerance develops

Answer 43

Short Acting β2 agonist - fast acting → stop asthma attack in progress - SM relaxation & stabilize mast cells -*more bronchodilation w/ fewer SE than albuterol SE: Tachycardia, nervousness & dizziness, tremor --short lived

Answer 44

Long acting β2 agonist (DoA 12 hours) - SM relaxation & stabilize mast cells - used **prophylactically - take 20 min to take affect - -not for relief of Asthma attack in progress -given w/ corticosteroid long term → ↑ sensitivity SE: Tachycardia, nervousness & dizziness, tremor - -short lived - tolerance develops → down regulation of β2 receptors

Answer 45

Muscarinic antagonist (why are SE minimal) - not absorbed systemically → stay in lung (4ry ammonium) - treat **COPD or Emphysema - brochodilation develops more slowly than w/ β2 agonist SE: cough, dry mouth, nausea -potential ↑ in intraocular pressure Tiotropium → longer DoA; 1x day use

Answer 46

Brochodilator - blocks adenosine receptors → ↓ bronchoconstriction & inflammatory mediators - PDE inhibitor → ↑ cAMP → SM relax (Bronchodilation) - -stimulated cardiac muscle -low therapeutic index: OD → arrhythmia & seizures - Phenytoin, rifampin, smoking, OC → ↑ clearance - Cimetidine & erythromycin → ↓ clearance SE: CNS → nervousness & insomnia (like caffeine) Cardiac → ionotropic & chronotropic→ tachycardia → arrythmias Muscle → ↑ contractility of diaphragm ↓ fatigue weak diuretic

Answer 47

Inhaled Corticosteroids - ↓ inflammation and ↑ sensitivity to β agonist - -effects begin w/in 1 week - -very few side effects --oral steroids for severe cases to bring symptoms under control SE: oralpharyngeal candidiasis - hoarsness - small ↓ in bone density

Answer 48

Leukotriene Inhibitor - Block Leukotriene receptor - -↓ asthmatic response to exercise & cold air - -↓ need for steroids Zileuton - blocks 5-lipoxygenase → ↓ synthesis of LT - -many ↓ asthma related to Aspirin or NSAIDS - must be taken chronically - will not stop an asthma attack in progress SE: ↑ upper respiratory infections, sore throat, sleepiness

Answer 49

Asthma treatment - IgE antibody → prevents binding to mast cells & basophils - PREVENT allergic reactions -SubQ injections → serious allergic & skin reactions

Answer 50

NOT a bronchodilator - ↓ RELEASE of histamine from mast cells & prevent B-spasm - treats asthma, esp. in CHILDREN - used several times a day for prophylaxis SE: BAD TASTE

Answer 51

Sedating antihistamine (1st gen H1 antagonist) - significant anti-ACh → motion sickness - ↓ itch, Lewis triple response (flus, flare, wheal), edema - ↓ salivary & lacrimal secretion - small ↓ in bronchospasm - small ↓ in vasodilation (H2 is still causing dilation) **Promethazine → anti-emetic (DA, Musc, H1) SE: - sedation and ↓ motor skills - CI in children - dryness of mouth, urinary retention, constipation - Teratogenic - ↓ seizure threshold - GI distress → ↓ if given w/ food -AVOID Alcohol & CNS depressants OD → atropine poisoning (excitement, convulsions, fixed dilated pupils)

Answer 52

Non-sedating antihistamine (2nd gen H1 antagonist) - do not enter brain → mainly peripheral receptors - NOT anti-ACh - -non-sedating & fewer side effects - ↓ itch, Lewis triple response (flus, flare, wheal), edema - small ↓ in bronchospasm - small ↓ in vasodilation (H2 is still causing dilation) -better at PREVENTING allergic rxn than treating them - Teratogenic - ↓ seizure threshold - GI distress → ↓ if given w/ food - AVOID Alcohol & CNS depressants - Erythromycin & Ketoconazole may ↓ metabolism (3A4) OVERDOSE → cardiac arrhythmias

Answer 53

Non-sedating antihistamine (2nd gen H1 antagonist) - ONLY eliminated by the KIDNEY - -avoid drug interactions or liver disease - may inhibit release of histamine from mast cell

Answer 54

Nasal H1 antagonist Non-competative H1 blocker -↓ RELEASE of histamine from mast cells -Allergic rhinitis

Answer 55

Acid-neutralizing agent / Osmotic laxative - Magnesium→ ↑ gastric motility → diarrhea - Aluminum → relax SM & ↓ gastric motility → constipation - -combine to cancel out effects - less absorption than bicarbonates - form complexes and ↓ absorption of iron other drugs - ↓ bioavailability of phenytoin, digitalis, propranolol - alkalize urine → ↑ elimination of salicylate & phenobarbital -toxicity may occur if renal function impaired

Answer 56

H2 antagonist - Block H2 → ↓ H+,K+ ATPase pump → ↓ H+ ions - -most effective ↓ NOCTURNAL acid formation - treatment: duodenal & gastric ulcers, GERD, ZE syndrome - pre-op → ↓ acidity incase of aspiration - prevent development of stress ulcers * *Severe allergic reactions → ↓ H2 mediated vasodilation along w/ H1 antagonist SE: headache, dizziness, nausea -↓ bioavailability of drugs absorbed at low pH CIMETIDINE - chronic high doses → anti-androgen effect - -↓ libido, impotence, impotence - - treat masculinization (hirsutism) - Inhibits CYP3A → ↓ metabolism of many drugs - -warfarin, phenytoin, theophylline, phenobarbital, digoxin, quinidine, TCA, propanolol, nifedipine

Answer 57

PPI - Irreversibly inhibit H+,K+ ATPase pump - prodrugs → become active & trapped in Parietal cells only - -highly lipophilic - takes 2-5 days for full effect → lasts 1-2 days - given for long periods -- 1-2 months - take on empty stomach ~30 min before meal - best absorbed at alkaline pH - DOC: GERD w/ esophagitis - prevent GERD - gastric & duodenal ulcers (prevent due to NSAIDS) - high doses → Zollinger-Ellison syndrome Adverse: - GI effect: nausea, diarrhea, abdominal colic - ↓ absorption of Calcium & Magnesium - ↑ cough & URT infections (Pneumonia) Omeprazole inhibits CYP2C19 → ↓ metabolism of - -Phenytoinm diazepam, *warfarin, - inhibits conversion of Clopidogrel

Answer 58

Cytoprotective agent (PG analog) - PG E1 analog → ↑ secretion of mucus & ↓ acid - prevents ulceration due to NSAIDS CONTRA → PREGNANCY → can induce contractions and cause abortion

Answer 59

Prokinetic agent (D2 antagonist) - blocks D2 → ↑ ACh release → ↑ motility & tone - Antiemetic → acts on chemoreceptor trigger zone * *Side effects: - high doses → extrapyramidal symptoms, exacerbation of Parkinson's CI in pregnancy → methemeglobinemia in neonates

Answer 60

Antispasmodic (Antimuscarinic) - Block M3 → ↓ intestinal overactivity, cramping, spasm - -slightly ↓ acid secretion from ↓ Vagal activity -SE: dry mouth, sedation, constipation TCA → anti-muscarinic → treat IBS

Answer 61

Anti-nausea / -emetic--Serotonin antagonist - Selectively blocks 5HT3 receptors in CTZ & GI tract - prevent vomiting due to - -Chemotherapy & vagal stimulation - -NOT effective → motion sickness

Answer 62

- 5HT3 - D1 - Neurokinin 1 - Opioid receptors

Answer 63

Bulk-forming Laxative SE: bloating and flatulence

Answer 64

Laxative - stimulates peristalsis by action on mucosa of colon - very mild

Answer 65

Osmotic Laxative - disaccharide that can't absorbed → ↑ osmotic pressure - metabolized by colonic bacteria → lactic acid - -gas, flatulence, abdominal dissension - acidic environment → ionized ammonia to ammonium - -traps it in colon → ↓ ammonia build-up w/ cirrhosis

Answer 66

Osmotic Laxative -used in prep for colonoscopy or intestinal procedures

Answer 67

Anti-Constipation (PGE1 derivative) - activates ClC-2 Cl- channels → ↑ intestinal fluid secretion - -softens stool & ↑ intestinal motility - reduces symptoms of chronic constipation - -bloating, straining, hard stools - doesnt alter electrolyte concentrations

Answer 68

Antidiarrheal (opioid derivative) - ↓ peristalsis by constrict circular m. & relax longitudinal m. - -NO CNS effect → low abuse potential CI: - diarrhea due to organisms that penetrate intestinal mucosa - -allows more time to invade - Ulcerative colitis → toxic megacolon

Answer 69

Antiflatulent -coats & dissipates gas

Answer 70

Somatostatin analogue - ↓ release of gastrin, CCK, serotonin, histamine - -↓ intestinal & pancreatic secretion - -↓ GI motility & gallbladder contraction - -↓ portal & splanchnic blood flow Treats carcinoid & VIP tumors

Answer 71

- absorbs excess water - -may absorb some microbial toxins - -may destroy some pathogens - Salicylate → ↓ PG synthesis → ↓ secretion & anti-inflamm - Treats travelers diarrhea & other non-specific causes CI: salicylate allergies & children → Reye syndrome

Answer 72

Cytoprotective - polymerizes in stomach acid → binds epithelium & exposed proteins from ulcer - → forms a PROTECTIVE barrier - may cause constipation → ALUMINUM

Answer 73

N-acetyltransferase 2 gene -transfers acetyl to amine → amide on drug Qualitative not quantitative difference <>Slow acetylator alelle → recessive (r/r only) - -Lupus → procainamide & hydralazine - -Hepatoxoicity → isoniazid <>Rapid acetylator allele → dominant (R/r or R/R) --Isoniazid, hydralazine, procainamide, sulfonamide, dapsone

Answer 74

second most important P450 enzyme -SSRI, TCA, opioids Metabolizers -poor, intermediate, extensive (normal), ultra-rapid

Answer 75

- H1 → Gq → SM, endothelium, hypothalamus - H2 → Gs → stomach, SM, heart, brain - H3 → Gi → presynaptic in brain - H4 → Gi → leukocytes in BM & blood

Answer 76

- vasodilation → hypoTN & shock (H1 & H2) - tachycardia - edema (H1) - bronchospasm & ↑ secretions of lung (H1) - ↑ gastric acid & pepsin - ↑ catecholamine in high doese - flush, flare, wheal