Do h2antagonists go thru first pass

Yes, cimetidine/ranitidine/famotidine go thru with 50% bioavailability- nizatidine has little first pass metabolism. Katzung 1083.

Physiology of acid secretion part 1

Vagal nerve stimuli of acetylcholine and gastrin release into blood bind to parietal cell receptors increasing calcium and stimulating proton pump acid secretion. Katzung 1081.

Physiology of acid secretion part 2

Gut endocrine cells ECL gastrin and acetylcholine receptors stimulate histamine release which binds to h2 receptor on parietal cells increasing cAMP which stimulates acid secretion. Katzung p 1082.

Use antacids cautiously with what diseases

Renal failure, heart failure, or HTN. Katzung p1083.

Pharmacodynamics of h2 inhibitors

Competitive Antagonists inihibitors parietal cell h2 receptors and suppress basal and meal-stimulated acid secretion, dose dependent. P 1084.

Administration of h2 inihibtors

Work best for nocturnal acid secretion. Greatest coverage for 10hrs so give twice daily, take before meals. P 1084.

Which promotes better ulcer healing: PPI or H2 antagonist

PPI- so give if some if it takes NSAIDS and gets ulcers p. 1085.

How should h. Pylori be treated

14-day PPI 2xdaily; clarithromycin, 500mg BID, & either amoxicillin 1gm BID, or metronidazole 500mg BID. Then PPI daily for 4-6 wks. p 1085.

When would u give h2 antagonists with h. Pylori

For the minority of pt that h. Pylori is not eradicated, may give h2 antagonist at bedtime for ulcer prevention p. 1085.

Drug interactions of h2 antagonists

Interferes with P450, will prolong half life of drugs with this metabolism pathway. P. 1085 katzung

Adverse effects of h2 antagonists

Mental status changes, nosocomial pneumonia, gynecomastia, male impotence, galactorrhea in women, possible blood dyscrasias, cross placenta and breast milk. P. 1085 katzung.

Pregnancy category of PPI

No harm to animal fetus but no test on human, cat B? P, 1088.

Nutritional adverse affects of PPI

Osteoporosis, life threatening hypo magnesia with secondary hypocalcemia if long term usage. P. 1088

What does PPI do to clopidegral/plavix

Reduce activation, p. 1089.

Neostigmine

Acetylcholinestetase inhibitor that enhances emptying p. 1092.

Adverse effects of metocloprsmdi de/zofran

Restlessness, drowsiness, insomnia, anxiety, and agitation p. 1092.

What antibiotic promotes gastric motility

Macrolides, erythromycin. katzung p. 1092

What are Bulk forming laxatives/polycarbophil

Indigestible, hydrophilic colloids that absorb water forming a bulky
Emollient gel that distends the colon/promotes peristalsis.

S/E of bulk-forming for laxatives/polycarbophil

Increased bloating and flatus, katzung p. 1093.

What are Osmotic laxatives

Soluble but nonabsorbable compounds that increase liquidity due to obligate increase fecal fluid. Katzung p. 1093.

What are purgatives

Mag citrate & sodium phosphate: they are high dose osmotics & produce evac in 1-3hrs. Katzung p. 1093.

Administration of polyethylene glycol/miralax

For bowel cleanse take 2-4L over 2-4 hours: to prevent constipation take 17gm mixed with water: does not produce cramps/flatus like sorbitol/lactulose. Katzung p. 1093.

Examples of anthraquinone derivatives stimulant laxatives

Aloe, senna, and cascara natural; in plants. Katzung p. 1093.

S/E of chronic anthraquinone derivatives

Brown colon "Melanosis coli". Katzung p. 1093

What laxative is safe for long term use

Bisacodyl katzung p 1093.

What are 2 selective antagonists of opioid receptor for opioid induced constipation

Methyl naltrexone bromide and albino pan. Katzung p. 1094.

When to use antidiarrheals

To control chronic diarrhea caused by conditions such as IBS & IBD. Katzung p. 1094.

When to not use antidiarrheals

Bloody diarrhea, high fever, systemic toxicity, or worsening symptoms. Katzung p. 1094.

What do you use for chronic and pain in IBS

Low dose of tricyclics antidepressants(amitryptiline) they affect gi motility and secretion reducing stool frequency and liquidity. Katzung p. 1096.

S/E of antispasmodic

Anti cholinergics effects, dry
Mouth, visual disturbances, urinary retention, and constipation. Katzung p. 1096.

What do 5-HT 3- receptor blockers affect/alosetron.

Nausea, bloating, pain, inhibits colon motility especially left colon increasing colonic transit time. Katzung p. 1096.

What is serious side effect of alosetron

Constipation: possibly requiring surgery. Katzung p. 1096.

What is primary action of 5-Asa/aminosakicylates

Blockade of prostaglandin synthesis by inhibition of cycloixygenas r. Katzung p. 1102.

What's considered first line of defense for ulcerative colitis

5-Asa, depending on location may need to give as enema or a mesalamine. P. 1102 katzung

What's the most common drug for IBD

Glucocorticoids/prednisone katzung not useful for maintaining remission p. 1103

What med is important in reduction and maintenance of ulcerative colitis and chrons

Azathioporine and 6-mp

What are advers effects of azathioporine and 6-mp

N/v, bone marrow suppression, and hepatic toxicity: lab monitor with cbc and liver fx katzung p. 1104

what is gonadarche

the change in ovarian function at puberty thereby begins estrogen production to induce endometrial changes and periodic bleeding. katzung p. 715

what triggers ovulation

follicles begin to enlarge in response to FSH; 5-6 days the dominant follicle enlarges and cells multiply due to LH; the cells synthesize and release estrogen which inhibits FSH release; the estrogen reaches a peak mid cycle (14 days) and the granolas cel

what are the major estrogens produced by women

estradiol, estrone, estriol. katzung p. 717

which estrogen is excreted in urine and can be tested to assess fetal well-being

estriol, katzung p. 717

pharmacokinetics of estrogen

binds strongly to alpha2 globulin, low affinity for albumin, bound estrogen is unavailable for diffusion into cell; converted into estriol and estrone by liver; excreted in bile; crosses breastmilk; minimize first pass affect to reduce risk for increase c

what are 2 types of preparations for oral contraceptives

1. combo of estrogen and progestins. 2. continuous progestin without concomitant estrogen. katzung 726.

what are 3 categories of combo OC

monophasic- constant dosage of both components.
biphasic and triphasic- dose of 1 or both components is changed 1-2 times during cycle. katzung 726.

effects of OC on uterus

after long usage some hypertrophy and polyp formation. cervical mucus may be thicker and less copious. OC with smaller amts of estrogen may produce more glandular atrophy and less bleeding. katzung 727.

effects of OC on breasts

stimulation and some enlargement may occur especially when on estrogen containing OC. lactation suppression, so give in some doses. katzung 727.

mechanism of action of OC

selective inhibition of pituitary function and in turn inhibits ovulation. katzung 727

are estrogens a feel good hormone

yes, they are even being used to treat postmenapausal tension, post partum depression, and climacteric depression. katzung 727.

effects of OC on blood

anemis, folic-acid anemias, thrombus, increase iron, increase blood clotting. katzung 727.

effects of OC on liver

alterations in hepatic drug excretion. reduce bile flow and may cause increase in gallbladder disease. katzung 728

effect of OC on carb metabolism

reduce the rate of carb absorption. increase insulin level. cause carb intolerance. katzung 728

effects of OC on cardiac

increase cardiac output and b/p. katzung 728

effects of OC on skin

progestin OC increase sebum production and in turn hair growth, darken skin color, acne
estrogen OC decrease sebum production. katzung 728

what meds can decrease effectiveness of OC

antibiotics that affect hepatic metabolism or phenytoin. katzung 728

mild adverse effects of OC- usually no dc meds necessary

too much estrogen: Nausea, mastalgia, bleeding, edema.
migraines, increase sed rates, change in serum proteins, evaluate thyroid, adrenal, and pituitary function. katzung 728

moderate adverse effects of OC- may need to dc meds

breakthrough bleeding-biphasic and triphasic decrease breakthrough bleeding. weight gain- may need to decrease progesterine, bacteriuria d/t ureteral dilation. katzung 729

severe adverse effects- dc meds

thromboembolism r/t estrogen content, MI d/t glucose intolerance/decrease HDL/increase LDL/increase platelet aggregation. katzung 729

contraindications of OC

hx of cardiac disease, thrombi, undiagnosed heavy vaginal bleeding, breast tumors, estrogen dependent neoplasms, liver disease, eczema, migraines, diabetes, optic neuritis. katzung 730

when wold progestin only be helpful

puts with hx of hepatic disease, HTN, psychosis, mental retardation, or thrombi. katzung 730

Pre-htn

120-135/80-89. Katzung 170

Htn

140/90. Katzung 170

Stage 1 htn

140-159/90-99. Katzung 170.

How do diuretics work

Deplete body of Na and reducing blood volume. Katzung 171

How do sympathoplegic agents work

Reduce peripheral vascular resistance, inhibit cardiac function, and increase venous pooling. Katzung 172

How do direct vasodilators work

Relax smooth muscle, thus dilating resistance vessels. Katzung 172

How do Angiotensin blockers work

Reduce peripheral vascular resistance. Katzung 172.

When would a powerful loop of henle diuretic/furosemide be used

Severe htn when multiple drugs with Na retaining properties are used; in renal insufficiency when glomerular filtration rate less than 30-40ml/min; cardiac failure or cirrhosis which Na retention is marked. Katzung 173.

What drugs can increase blood pressure

Sympathizing tic decongestants, NSAIDS, oral contraceptives, and some herbal mess. Katzung 186.

Stage 2 htn

160/100. Katzung 170.

What are the prototype drugs of loop diuretics

furosemide & ethacrynic acid p. 258

What are sulfonamide loop diuretics

Bumetanide & toresmide. pg 258

Pharmacokinetics of loop diuretics

rapidly abosrobed and excreted through the kidneys. effects last for about 2-4hrs. NSAIDS or probenecid may reduce secretion of loop diuretics. p. 258

pharmacodynamic consideration of loop diuretcis

may cause increase in calcium and mag excretion increasing risk for hypomagnesemia but not hypocalcemia due to vitamin d induced intestinal absorption and parathyroid renal asbsorption may be increased. p. 259

What are indication of use of loop diuretics

pulmonary edema, edematous conditions, acute hypercalcemia; hyperkalemia, acute renal failure, and anion overdose. p. 259

Clinical use for thiazides

HTN, heart, failure, nephrolithiasis D/T idiopathic hypercalciuria, nephrogenic diabetes insipidus. p. 261

effects of thiazide toxicity

hypokalemia metabolic alkalosis and hyperuricemia, impaired carb tolerance/hypoglycemia, hyperlipidemia, hyponatremia, sulfa cross-sensitivity, rash, photosensitivity, weakness, fatigue, impotence. p. 261

prototype drug for k+ sparing diurectics

spironolactone/eplerenone or amiloride/triamterene. p. 261.

what is spironalactone

competitive antagonist of aldosterone with a slow onset needing several days before full therapeutic effect.