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Pharm Spring Block I chart notes
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174
Pharmacology
Graduate
02/13/2013

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Term
What is calcitriol?
Definition
The active form of Vit D
Term
What are normal VitD values?
Definition
Normal value is 30ng/ml
Need 1000-1500 units/day
Term
Secretion of calcitonin is stimulated by what?
Definition
Gastrin
Hypercalcemia
Term
Hypercalcemia is defined as what?
Definition
Ca++ > 10.5mg/dL
Term
How is hypercalcemia treated?
Definition
IV fluids
Excretion using loop diuretics w/ Furosemide
Calcitonin -> drug of choice for CHF patients
Long term treatment: Pamidronate, Etidronate, Zoledronate
Term
Hypocalcemia is defined as what?
Definition
Ca++ < 8.5mg/dL
Term
All Ca++ supplements require what?
Definition
An acidic environment for absorption except calcium citrate
Term
What is the drug of choice for the treatment of hypocalcemia?
Definition
Calcium gluconate due to minimal irritation to veins
Term
What are second line treatments for hypocalcemia?
Definition
Calcium chloride
Calcium carbonate and Calcium lactate (Oral only)
Term
What does chronic glucocorticoid treatment do to calcium levels?
Definition
Down regulates Ca++ binding protein, inhibits Vit D activation, can cause osteoporosis. Give bisphosphonates (alendronate)
Term
How do you treat Paget's disease?
Definition
Bisphosphonates and calcitonin
Term
What is first line for the treatment of osteoperosis?
Definition
Bisphosphonates - Alendronate
Term
What is the MoA of bisphosphonates?
Definition
Anti-resorptive action inhibits action on osteoclasts
Changes expression of RANK-L
IV only, poor oral absorption
Term
What are the adverse effects of bisphosphonates?
Definition
GI bleed, GI irritation, contraindicated in GERD, peptic ulcers, renal dysfunction
Term
What are the bisphosphonates formulations?
Definition
Alendronate, Ibandronate, Pamidronate, Tiludronate, Risedronate, Etidronate sodium
Term
What are the calcitonen formulations?
Definition
Gibacalcin (human) and Calcimar (salmon)
Term
What are the adverse effects of Gibacalcin and Calcimar (calcitonen formulations)
Definition
Headache, weakness, nausea, vomiting, contraindicated with allergy, renal dysfunction
Term
What is the MoA of Plicamycin?
Definition
Cytotoxic antibiotic, inhibits hypercalcemic action of VitD and PTH
Highly toxic, limite duse
Term
What is Plicamycin used for?
Definition
Hypercalcemia due to advanced neoplasms
Term
Rickets, osteoporosis, and osteomalacia all require what for treatment?
Definition
VitD
Term
What are the VitD formulations?
Definition
Calcitriol
Ergocalciferol
Doxercalciferol
Term
What is calcitriol?
Definition
VitD3, activated form of VitD, given for patients with kidney failure
3-5day duration
Term
What are the contraindications for calcitriol use?
Definition
Hypercalcemia, patients on cardiac glycosides
Term
What is ergocalciferol?
Definition
VitD2
Given for hypophosphatemia, osteomalacia, osteoporosis, rickets
2 month duration
Term
What is doxercalciferol?
Definition
Vit D2 analog
Term
What are the indications for doxercalciferol use?
Definition
Given for hyperparathyroidism (reduces PTH)
Term
Doxercalciferol is contraindicated in what cases?
Definition
Pregnancy, hep and renal dysfunction
Term
What is Cinacalet?
Definition
A Calcimimetic, mimics Ca++ at Ca++ receptors of the parathyroid
Increased sensitivity to calcium to reduce PTH
30-40hr half life, long
Term
What is the only drug to shut out the parathyroid hormone release by binding the ionized calcium receptor?
Definition
Cinacalcet
Term
What is Teriparatide?
Definition
Recombinant form of PTH
Term
Patient with osteoporosis has failed bisphosphonates and estrogen modulators, T score is beyond 2.5. What do you use?
Definition
Teriparatide
Term
Teriparatide therapy beyond 21 months runs the risk of what?
Definition
Osteosarcoma formation
Term
What is Raloxifene
Definition
Selective estrogen receptor modulator used in the management of osteoporosis
Term
What are the Growth Hormone agonists?
Definition
Somatotropin
Somatrem
Term
What is Somatotropin? Uses?
Definition
Recombinant GH, given for GH deficiency, AIDS wasting
Term
What is Somatrem?
Definition
GH with additional methionine at terminus, given for GH def and AIDS wasting
Term
What is Sermorelin?
Definition
GHRH agonist, somewhat less effective than somatotropin, given for the same reasons
Term
What are the somatostatin agonists?
Definition
Octreotide
Pegvisomant
Term
What are the actions of somatostatin?
Definition
Inhibitory hormone, inhibits anterior pituitary and GI hormones
Term
What are the actions of Octreotide?
Definition
 Similar to somatostatin but longer ½ life
Selectively inhibits growth of prolactin secreting adenomas to somatostatin receptors SSTR2 and SSTR5
Inhibits secretion of GH, serotonin, gastrin, VIP, motilin
Can cause gallstones
Term
What are the actions of Pegvisomant?
Definition
Mutant of GH that binds GH receptor and induces internalization without activating the receptor
Contraindicated in liver dysfunction
Term
What are the dopamine D2 receptor Agonists
Definition
Bromocriptine, Pergolide, Cabergoline
Term
What are the actions of Bromocriptine, Pergolide, Cabergoline?
Definition
Dopamine D2 receptor agonists
Stops growth of prolactin secreting adenomas
Decreased dopamine release in parkinson’s
Causes postural hypotension due to vasodilation of renal vascular beds
Term
What are the GnRH agonists?
Definition
Gonadorelin, Gosrelin, Nafarelin (nasal spray)
Term
What affects of Gonadorelin, Gosrelin, Nafarelin (GnRH agonists) on LH and FSH secretion?
Definition
Pulsatile administration = release of FSH and LH
Non-pulsatile administration = FSH and LH “flare” then inhibition after 7 days
Used to either stimulate or (more often) suppress gonadotropin release
Can be given to suppress ovulation, limit 6 months, used for endometriosis
Contraindicated in pregnancy and breast feeding
Term
What are the GnRH antagonists?
Definition
Ganirelix and Cetrorelix
Term
Ganirelix and Cetrorelix are used to treat what?
Definition
Given to delay ovulation in women undergoing fertility treatment, suppress cancer growth
Term
What is the MoA of Ganirelix and Cetrorelix?
Definition
Given via subcutaneous injection
Acts as GnRH antagonist to prevent LH surge during ovarian hyperstimulation
Duration of administration is slower, less negative impact on ovarian response
May cause ovarian hyperstimulation syndrome
Term
What are the FSH agonists?
Definition
Urofollitropin, Follitropin alpha, Follitropin Beta
Extracted from the urine of postmenopausal women
Term
What is Lutropin?
Definition
Leuteinizing hormone agonist, all given subQ or IM, is recombinant human LH
Term
Lutropin is only given alongside what drug?
Definition
Follitropin alpha for stimulation of follicular development in infertile women with profound LH deficiency
Term
What are the hCG agonists?
Definition
Propasi, Pregnyl, Choriogonadotropin alpha
Term
Oxytocin is given for what purpose?
Definition
Induce labor and prevent postpartum bleeding, at high concentrations acts as antidiuretic. May cause fetal distress, placental abruption, uterine rupture, fluid retention
Term
What are the actions of Vasopressin?
Definition
Activates receptors in collecting tubules leading to increased water resorption
V2-like receptor activity at extrarenal sites regulates release of coagulation factor VIII and von Willebrand factor
Term
What is Desmopressin?
Definition
Long acting synthetic analog of Vasopressin, mainly acts at V2 receptor
Term
What is Conivaptan?
Definition
Vasopressin antagonist used to treat hyponatremia assoc w/ elev. vasopressin
Term
Ghrelin induces the secretion of what?
Definition
GH
Term
What is the function of prolactin?
Definition
Activates JAK-STAT signal pathway to increase casein production for milk production and breast development during pregnancy
Term
What are the Thionamides?
Definition
Methimazoleb and Porpylthiouracil
Term
What is the function of Methimazoleb and Porpylthiouracil?
Definition
Reduces synthesis of thyroid hormones, inhibits thyroperoxidase to reduce iodination of tyrosyl residues
Antithyroid action delayed days-weeks until existing stores of T3/4 are depleted
Short half lives
May cause arthralgia, fever, rash, fetal goiter, etc
Term
What is the preferred drug for the treatment of fetal thyrotoxicosis?
Definition
Methimazoleb
Term
What is the drug of choice for the treatment of thyroid storm and hyperthyroidism in pregnancy?
Definition
Propylthiouracil
Term
Potassium iodide is used for what?
Definition
Oral solution only, used in treatment of thyroid storm and to prepare hyperthyroid patients for thyroidectomy. Not good long term therapy
Term
What are Iopanoic acid and Lopadate?
Definition
Iodinated contrast agents that prevent the release of T4 and T3 as well as the conversion of T4 to T3
Term
What are Iopanoic acid and Lopadate used for?
Definition
Temporary treatment of highly toxic thyrotoxic patients, used in subacute thyroiditis and patients intolerant to thionamides
Term
First line treatment of Graves disease includes what?
Definition
Radioiodine (Iodine131)
Term
What is Armour USP?
Definition
Natural thyroid extract mixture of T4/T3 from animals, unpredictable ratio and effect, possible hypersensitivity
Term
What drug is first line for the treatment of hypothyroidism?
Definition
Levothyroxine Sodium
Term
What is Levothyroxine Sodium?
Definition
Synthetic T3, well absorbed orally, fast onset of action, half dose of T4 needed
Term
What is Liotrix?
Definition
T4/T3 mix not preferred, expensive
Term
Testosterone is converted to what?
Definition
to DHT, a more potent form, via 5alpha-reductase
Term
What is the difference between type I and II 5alpha-reductase?
Definition
Type I 5-alpha-reductase found in non-genital skin, liver, and bone
Type II 5-alpha-reductase found in genita skin
Term
Testosterone is normally bound to what?
Definition
Androgen binding protein, sex hormone binding globulin (SHBG), and albumin
Term
Histeron and Androderm are used in what?
Definition
Testosterone patches that bypass first pass metabolism
Term
What are the testosterone esters?
Definition
Testosterone enanthat and Testosterone cypionate
Given via IM, highly lipophilic, given every 2 weeks
Term
What are the 17alpha alkylated androgens aka anabolic steroids?
Definition
Methyltestosterone, Oxandrolone, Stanozolol, Danazol
Causes hepatotoxicity given PO
Term
What is Tetrahydrogestrinoneb
Definition
newer androgen formulation
Term
What are the uses for testosterone therapy?
Definition
Male hypogonadism, male andropause, female hypogonadism, improve libido, enhance athletic performance, male contraception, muscle wasting in AIDS, anaplastic anemia
Term
What androgen drug used as adjunctivent for hemolytic anemia and drug induced TTP?
Definition
Danazol
Term
What are the side effects of testosterone treatment?
Definition
Decreased testicle size, increased RBC production, gynecomastia, decreased HDL, increased LDL, advancement of BPH or prostate cancer
Term
What are the GnRH/LHRH agonists?
Definition
Buserelin, Leuproreline, Goserelin, Nafarelin
Term
What are the actions of Buserelin, Leuproreline, Goserelin, Nafarelin?
Definition
GnRH analogs that desensitize the GnRH signaling pathway, inhibiting the release of LH and FSH
Term
Buserelin, Leuproreline, Goserelin, Nafarelin (GnRH agonists) are used for what treatment?
Definition
BPH and hirsutism treatment
Term
What is Abirelix?
Definition
GnRH antagonist with extended release used to treat prostate cancer
Significant incidence of hypersensitivity reactions
Term
What are the androgen receptor antagonists?
Definition
Flutamide, Bicaltamide, Nilutamide, Spironolactone, Cyproterone acetate
Term
What is the MoA of Flutamide, Bicaltamide, Nilutamide, Spironolactone, Cyproterone acetate (androgen receptor antagonists)?
Definition
Limited efficacy when used alone
Blocks negative feedback on HPA axis to increase LH secretion and promote testosterone promotion, takes 6-9 months to reach maximal effect, avoid donating blood
Causes hepatotoxicity and possible gynecomastia (spironolactone)
Term
GnRH analogs are used alongside which to treat metastatic prostate cancer?
Definition
Androgen receptor antagonists:
Flutamide, Bicaltamide, Nilutamide, Spironolactone, Cyproterone acetate
Term
Flutamide, spironolactone, cyproterone acetate are used with estrogen to treat what?
Definition
Hirsutism in women
Term
Finasteride (Type I) and Dutasteride (Type I and II) are what type of drugs?
Definition
5-alpha reductase inhibitors, blocks the conversion of destosterone to DHT
Term
Finasteride (Type I) and Dutasteride (Type I and II) are used for what?
Definition
5-alpha reductase inhibitors, blocks the conversion of destosterone to DHT
Used for benign prostatic hyperplasia
Term
What is first line for the treatment of BPH?
Definition
Alpha-1 blockers: Terazosin, Doxazosin, Tumulosin, Alfuzosin
Increased urine flow within 48hrs, decreased ejaculation, Alfuzosin prolongs QT interval
Term
Which phase of menstruation is gonadotropin dependent?
Definition
Basal growth phase
Term
Follicles are extremely sensitive and dependent on what hormone during which phase?
Definition
FSH during the rapid growth phase. Drop of FSH causes atresia with the exception of the dominant follicle
Term
What are estrogen's effects on the liver?
Definition
Improves lipid profile, increases synthesis of binding proteins SHBG, CBG, and TBH, increases synthesis of coagulation factors
Term
What is estrogen's effect on adipose tissue?
Definition
Decreases adipose tissue, inhibiting LPL and increasing activity of hormone sensitive lipase
Term
What effect does estrogen have on kidney function?
Definition
Natriuretic effect on kidneys as a competitive inhibitor of aldosterone
Term
Estrogen from the ovaries induces which phase of menses?
Definition
Proliferative phase of the endometrium
Term
What is the principal estrogen in circulation?
Definition
Estradiol
Estrone is the main estrogen synthesized by the adrenal gland
Both estradiol and estrone can be converted to estriol
Term
What is the monophasic combined pill?
Definition
Lovoral, Allesse
Term
What is the biphasic combined pill?
Definition
Orthonovum (rarely used)
Term
What is in the combined pill?
Definition
Has 3 generations, contains synthetic estrogone: ethinyl estradiol or mestranol and a variety of C-19 progestin steroids: **Norgestrel, Norgestimate, **Desogestrol, Levonorgestrel, Ethynodiol diacetate, Norethindrone acetate
Term
What metabolizes OCCs?
Definition
CYP450, beware drug interactions
Term
Contraceptive failure occurs when mixed with what drugs?
Definition
Rifampin, carbamazepine, phenytoin
Term
What are side effects of the combined pill?
Definition
ACHES = Abdomen Chest Headaches Eye Severe leg pain
Gallstones, blood clots, pancreatitis, stroke, HTN, migraine, occlusion, DVT
Detrimental effects on lipid panel, impairs glucose tolerance, increased risk of breast carcinoma
Term
The combined pill is contraindicated under what risk factors?
Definition
Heavy smoker, HTN, undiagnosed vaginal bleed, diabetes with vascular complications, DVT or PE, history of stroke, history of thrombosis, history of breast cancer, active viral hepatitis or cirrhosis, breastfeeding, major surgery with immobilization, history of cholestasis with COC use, pregnancy
Term
What is Depot Provera?
Definition
Long acting progesterone via IM injections, infertility persists for months
Term
Progestin implants use what formulations of progestin?
Definition
Levonorgestrel or etonorgestrel, cheaper, lasts for months
Term
What are the post-coital contraceptives?
Definition
Ovral, Plan B, Preven
High dose of progesterone, main effect is to make environment inhospitable to sperm
Term
What is the leading cause of death related to menopause?
Definition
Coronary artery disease
Term
What are the conjugated Equine Estrogens?
Definition
Cenestin, Enjuvia, Premarin, Progens
Term
The conjugated Equine Estrogens are used to treat what?
Definition
Primary ovarian failure, menopause symptoms, dose not reduce risk of CHD
Include progestin in women with intact uterus to lower risk of endometrial cancer
Term
What are the esterified estrogens?
Definition
Estratab, Menest, Menrium, Neo-estrone
Given for primary ovarian failure, menopause symptoms, dost not reduce risk of CHD
Include progestin in women with intact uterus to lower risk of endometrial cancer
Term
What is Clonidine used for?
Definition
Alpha-2 antagonist used to reduce hot flashes
Term
What is Desvenlaflaxine used for?
Definition
SSRI used to reduce hot flashes
Term
What are the aromatase inhibitors? What are they used for?
Definition
Anastrozol and Letrozole used to treat endometriosis
Term
What is the MoA of Prochlorperazine?
Definition
A phenothiazine
Blocks dopamine receptors, moderates chemo agents
Causes sedation and extrapyramidal symptoms (parkinsons symptoms)
Term
What is the MoA of Ondansetron, Granisetron, Dolasetron?
Definition
5HT3 inhibitors
5HT3 receptor blockade in the vomiting center and chemoreceptor trigger zone, long duration of action, highly effective, dose adjust in cases of hepatic insufficiency
Term
What is the MoA of Metoclopramide?
Definition
Dopamine antagonist
Elevates CTZ threshold/nausea threshold, used for gastroperesis, prevention of chemo induced emesis, good for GERD
Avoid high dose due to extrapyramidal symptoms, never use long term
Term
What is the MoA of Diphenhydramine, Meclizine, Hyoscine?
Definition
H1 antihistamines
o Used in combo with other antiemetics, prevents motion sickness, limited use by sedation, urinary retention, dizziness
Term
Which H1 antihistamines is approved for use as an anti-emetic used in pregnancy?
Definition
Meclizine
Term
What is the MoA of Dronabinol?
Definition
Cannabinoid, inhibits vomit control mechanism, not often used
Term
What is the MoA of Psyllium?
Definition
A laxative for the small and large intestines, increases bulk and moisture content in stool, stimulates peristalsis
Used to prevent straining during defecation
May cause bowel obstruction if taken with insufficient liquid
Term
What is the MoA of Lactulose, Salin catharitics, Magnesium citrate?
Definition
Acts on colon and small intestine to retain ammonia and produce cholecystokinin, producing osmotic effect to stimulate bowel evacuation
Used in prevention and treatment of portal cystemic encephalopathy, constipation, evacuate colon before exam/surgery, accelerate parasite or poison excretion
May cause electrolyte disturbance
Term
What is the MoA of Senna?
Definition
Stimulates colon interstitial smooth muscles to increase peristalsis, used to facilitate diminished colonic motor response or evacuate colon before exam/surgery
Causes discolored urine, electrolyte depletion
Term
What is the MoA of Docusate?
Definition
A stool softener than lowers surface tension in the intestines, facilitates penetration of fat and water into stool
Used for short term constipation and to evacuate colon before surgery/exam
Term
What are the anti-diarrhea opiods?
Definition
Diphenoxylate
Loperamide
Term
What is the MoA of Diphenoxylate?
Definition
Inhibits mucosal peristaltic reflex-reduction of GI motility, metabolized to active metabolite Difenoxin
Maximal anti-diarrheal effects with minimum CNS effects
Combined with atropine to prevent abuse
Term
Diphenoxylate is combined with what when used?
Definition
Atropine to prevent abuse
Term
What is the MoA of Loperamide?
Definition
Opioid inhibition of GI peristalsis, prolongs transit time of intestinal contents
Indicated for non-specific diarrhea and IBD, has peripheral opiate effects but no CNS effects
Term
What is the MoA of Bismuth subsalicylate aka pepto-bismol?
Definition
Is an anti-secretory, anti-inflammatory, anti-bacterial that coats the GI tract, hydrolyzed in GI to salicylate
Inhibits prostaglandin synthesis and reduces hypermotility and inflammation
Term
What GI medication should be avoid if bacterial enteritis is expected?
Definition
Opiates Diphenoxylate or Loperamide
Term
What are the Aminosalicylates?
Definition
Sulfasalazine, Olsalazine, Balsalazine
Inhibits synthesis of prostaglandins and inflammatory leukotrienes
Term
What is first line for the treatment of IBD?
Definition
Aminosalicylates:
Sulfasalazine, Olsalazine, Balsalazine
Term
What are the Mesalamine compounds?
Definition
Pentasa, Asacol, Rowasa, Canasa
Term
What is the MoA Mesalamine compounds Pentasa, Asacol, Rowasa, Canasa?
Definition
Direct salicylates that don’t require break down, modulates inflammatory response, especially leukotrienes, inhibits TNF
Used for IBD, Crohn’s disease, Ulcerative colitis
Term
What are the GI immunosuppressants?
Definition
Azathioprine, 6-Mercaptopurine, Methotrexate, Cyclosporine, Infliximab
Term
What is the MoA of the Gi immunosuppressants Azathioprine, 6-Mercaptopurine, Methotrexate, Cyclosporine, Infliximab?
Definition
Inhibits purine synthesis, reduces GI inflammation, reduces need for long term corticosteroid use, slow onset
Used to treat IBD
Term
What should you do if aminosalicylates and corticosteid therapy for IBD fails?
Definition
Increase methotrexate while decreasing corticosteroids
Term
What is used for symptomatic treatment of severe Crohn’s?
Definition
Infliximab and TNF-alpha antagonists
Inhibits induction of proinflammatory cytokines
Term
What are the anti-depressants used to modulate pain effects of neurotransmitters, used for IBS?
Definition
Amitriptyline and Doxepin
Term
What SSRIs are used for IBS?
Definition
Paroxetine, Fluoxetine, Sertraline
Acts on 5HT1 and 5HT2 receptors to reduce visceral hypersensitivity, less side effects
Term
What is the MoA of Alosetron?
Definition
Modulates visceral afferent activity from GI, may improve abd pain, not commonly prescribed, only given for extreme conditions of IBS
Term
How is H. pylori diagnosed?
Definition
Uupper endoscopy, serologic ab detection, urea breath test, or stool antigen tests
Term
What is first line therapy for H. pylori?
Definition
Omeprazole + Clarithromycin + Amoxicillin/Metronidazole
Term
What is the combination therapy for H. pylori?
Definition
PPI + Metronidazole or amoxicillin + clarithromycin
Term
What is the bismuth based regiment for H. pylori?
Definition
Omeprazole + Bismuth subsalicylate + Metronidazole + Tetracycline/Amoxicillin/Clarithromycin
Term
What is given as maintenance therapy H. pylori?
Definition
Low dose H2 antagonist or PPI
Term
NSAID induced ulcers are best treated with what?
Definition
Omeprazole, Misoprostol is 2nd choice
First stop NSAID, move to COX-2, then Omeprazole
Term
What is the best treatment for GERD?
Definition
H2 antagonists and PPIs (Omeprazole)
Term
Treat Zollinger-Ellison Syndrome (hypersecretion due to gastrin secreting tumor) with what?
Definition
Omeprazole
Term
You should avoid taking antacids with what drug?
Definition
Quinidine, a 1a anti-arrhythmic, causes increased absorption
Term
What are the antacids?
Definition
Al Hydroxide + Mg, Mg hydroxide, Simethicone, Mg carbonate, Ca carbonate, Sodium bicarbonate
Term
What is the order of H2 antagonist potency?
Definition
Famotidine > Nizatidine > Ranitidine > Cimetidine
Term
What is the MoA of Cimetidine?
Definition
H2 antagonist, suppresses all phases of daytime and nocturnal basal gastric acid secretion, given for PUD
Decreased hepatic metabolism of warfarin, phenobarbital, phenytoin, diazepam, propranolol, very significant
Term
What is the MoA of Rantidine?
Definition
H2 antagonist, potential anti-ulcer, reduces gastric acid release in response to food
Short term treatment of active duodenal ulcer, used for maintenance therapy
Term
What is the MoA of Nizatidine?
Definition
H2 antagonist, Inhibits gastric acid secretion, used for active duodenal ulcer and maintenance therapy
Term
What is the MoA of Famotidine?
Definition
Potent competitive inhibitor of histamine at H2 receptor sites, reduces output of HCL
Term
What is the MoA of Omeprazole?
Definition
PPI, suppresses gastric acid secretion by inhibiting H/K ATPase
Converted in parietal cell canaliculi to active form, onset within 1hr, lasts for more than 24hrs, better eradication of H. pylori when given in combo with anti-bacterial
Inhibits CYP450, decreased elimination of phenytoin, diazepam, warfarin
Term
What are the PPIs with no drug interactions?
Definition
Lansoprazole, Eesomeprazole, Pantoprazole, Raberprazole
Term
What is the MoA of Lansoprazole?
Definition
PPI, similar to omeprazole, combined with anti-bacterials better
Term
What is Esmerprazole?
Definition
Isomer of omeprazole, converted to active form, substantial suppression of acid secretion
Term
What PPIs have no CYP450 interaction?
Definition
Pantoprazole, Raberprazole
Term
What is the MoA of ACTH?
Definition
Binds to Gs FA 294 to increase transport of cholesterol from outer micochondrial membrane to inner to initiate cortisol synthesis
Term
9alpha-flouro analogs Dexamethasone, Betamethasone, and Triamcinolone are mostly bound to what?
Definition
Albumin
Term
How do glucocorticoids cause the death of hypocampal cells?
Definition
Indirectly due to BP and electrolyte changes
Term
Cortisol is converted to inert cortisone at mineralcorticoid receptors by what?
Definition
11b-hydroxysteroid dehydrogenase
Term
What is the MoA of Ketconazole?
Definition
Inhibits all gonadal and adrenal steroid hormone synthesis, used to treat
Potential hypersensitivity and GI reactions
Term
What is the MoA of Metyrapone?
Definition
Inhibits 11-beta hydroxylase, increases adrenal androgens and aldosterol
Used to treat pregnant women with Cushings
Term
What is the MoA of Aminoglutethimide?
Definition
Inhibits conversion of cholesterol to pregnenolone to prohibit glucocorticoid synthesis
Used to treat Cushings due to adrenal carcinoma, ectopic ACTH producing tumors, adrenal hyperplasia
May cause lethargy, drowsiness, headache
Term
What is the MoA of Spironolactone?
Definition
Antagonist at mineralcorticoid receptor, used to treat hyperaldosteronism
Term
Primary adrenal insufficiency is treated with what?
Definition
Hydrocortisone or fudrocortisone 2/3 in morning, 1/3 in evening
Term
Secondary adrenal insufficiency refers to what?
Definition
Adrenals are working but suppressed due to low ACTH, often due to exogenous cortisol
Term
Fludrocortisone is another name for what?
Definition
Exogenous aldosterone
Term
What can given to prevent aromatization of androgens to estrogen?
Definition
Anastazole, Letrazole, Flutamide
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