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Spring Block 1 Drugs
all block 1 drugs
132
Medical
Professional
01/29/2013

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Term
Pamidronate
Definition
biphosphonate. locks into hydroxyapatite to antagonize PTH. Poor oral absorption. Given IV. CI'd in renal insufficiency.
Term
Alendronate
Definition
biphosphonate. locks into hydroxyapatite to antagonize PTH. Poor oral absorption. Given IV. CI'd in renal insufficiency.
Main use is for osteoporosis and glucocorticoid prophylaxis.
Term
Zoledronate
Definition
biphosphonate. locks into hydroxyapatite to antagonize PTH. Poor oral absorption. Given IV. CI'd in renal insufficiency.
Term
Cinacalcet
Definition
Ca mimetic. Used in hypercalcemia from tumors such as parathyroid tumors. Acts like free Ca to decrease PTH.
Displaces albumin bound verapamil, nsaids, and digoxin
Term
Ca Gluconate
Definition
IV elemental calcium. Preferred b/c it doesn't irritate the veins.
Term
Ca Chloride
Definition
irritates the veins.
Term
Ca carbonate
Definition
oral calcium
Term
Calcitriol
Definition
used in pts w/ renal failure.
Treats rickets, osteomalacia, and osteoporosis. CI'd in hypercalcemia or cardiac glycosides (aka digoxin)
Term
Vit D
Definition
used in rickets, osteomalacia, osteoporosis.
Term
Ergocalciferol
Definition
activated in the kidney to calcitriol. highly bound to albumin
Term
Doxicalciferol
Definition
same as ergocalciferol except that it is contraindicate in renal and hepatic dysfunction.
Term
Calcitonin
Definition
antagonizes PTH, inhibits Pagets bone turnover. Used in hypercalcemic emergencies.
SE - headaches, weakness, N/V on first dose
Term
Plicamycin
Definition
cytotoxic antibiotic. Inhibits actions of Vit D and PTH on osteoclasts.
Used for hypercalcemia from advanced tumors.
High toxicity. Only used in hospital.
Term
Teriparatide
Definition
recombinant PTH.
Only agent that stimulates new bone formation. Used if other treatment is failed.
If used over 21 months --> osteosarcoma
Term
Raloxifene
Definition
estrogen receptor agonist.
It is an agonist in the bbone and antagonist in the breast
Term
somatropin
Definition
GH mimetic. Mainly used for children SE - idiopathic intracranial HTN. increased incidence of leukemia. Scoliosis, slipped epiphysis. In adults -> peripheral edema, CTS, arthralgia, myalgia
Term
Mecasermin
Definition
Recombinant IGF-1. Used to treat pts with an GH receptor mutation.
SE - hypoglycemia
SE in adults -> peripheral edema, carpal tunnel, myalgia, arthralgia
Term
Octreotide
Definition

similar to SST. Inhibits GH, ST, Gastrin, VIP, and motilin. SE - N/D, bloating, gallstones, high and low blood sugar.

Treats acromegaly or gigantism

Term
Pegvisomant
Definition
GH receptor antagonist and thus inhibits IGF-1 production too. Causes internalizatin of GH receptor.
SE - liver damage
Term
bromocriptine
Definition
Dopamine receptor agonist (D2 specific)
Used to treat prolactinoma.
SE - N/V, headache, postural hypotension. nasal congestion
Gi coupled receptor on lactotrophs.
Term
cabergoline
Definition
used to treat prolactinoma
Less nausea than bromocriptine.
Gi coupled receptor on lactotrophs.
Term
gonadorelin
Definition
GnRH analog.
controls ovarian hyperstimulation. Suppresses LH surge, endometriosis, reduces T levels in prostate cancer. suppress precocious puberty.
SE - women->headache, menopause symptoms. men -> hot flashes, edema, dec libido, gynecomastia.
Term
goserelin
Definition
GnRH analogs. same as gonadorelin
Term
nafarelin
Definition
GnRH analogs. available in nasal spray.
Term
ganirelix
Definition
GnRH receptor antagonist. Prevent LH surge in ovarian hyperstimulation. used in cancers when you want to avoid LH surge such as prostate cancer.
Term
cetrorelix
Definition
GnRH receptor antagonist. Same as ganirelix.
Term
urofollitropin (follitropin)
Definition
FSH
Term
lutropin
Definition
LH. Only used with follitropin alpha in infertile females to stimulate follicular development when they are lH deficient.
Term
Propasi/Pregnyl
Definition
hCG preparation and is more commonly used then the LH preparation. What is the LH prep name?
Term
Oxytocin
Definition
Gq coupled receptor increasing intracellular Ca -> SM contraction.\
also activates PLC -> prostaglandins.
high doses induces vasopressor effect.
Used to induce labor and prevent post-partum bleeding.
SE - fetal distress, abruption, previa, fluid retention -> HF -> death
Term
vasopressin/Desmopressin
Definition
activates Gq V1 on vasculature and V2 on renal tubules (increased water reabsorption).
SE - abdominal cramping, HTN, arrhythmias, MI, and peripheral ischemia
Uses - esophageal variceal bleeding, polyuria, polydipsia, nocturnal enuresis.
Desmopressin - mainly activates V2 in kidneys.
Term
Thyroid USP (Armour)
Definition
hog/beef/sheep gland derived TH. Mix of T3 and T4. Unpredictable and possible hypersensitivity.
Term
Levothyroxine
Definition
Oral synthetic T4. Stable and is converted to T3 at a predictable rate.
Preferred treatment for hypothyroidism.
Food, Calcium, aluminum, antacids, and cholesterol resins interfere w/ absorption.
Metabolized by CYP3A4 (interferes w/ rifampin, phenytoin and phenobarbitol)
Takes 6-8 weeks for steady state levels.
initiate carefully in elderly pts. May require less.
Low Low doses in CVD.
overdose -> hyperthyroid symptoms and increased bone resorption -> osteoporosis
Term
Liothyronine sodium
Definition
Oral synthetic T3. Long half life. Fast onset of action. Treatment of choice for myxedemic coma (IV) Used in pts who can't convert T4 to T3. Higher incidence of cardiac side effects
Term
Liotrix
Definition
Synthetic T3 and T4
not preferred. Expensive
Term

thionamide.

Name 2

Definition

TH synthesis inhibitor

Methimazole

Propathiouracil

Term
Iodinated contrast agents
Definition
anti-thyroid drug. Effective temporary treatment of thyrotoxicosis for those who can't tolerate thionamides. Prevent T4 to T3 and release of TH.
Term
Radioiodine
Definition
causes ablation of the thyroid
Definitive graves treatment for pts w/ CVD, adenoma, and thionamides. Used to treat the ***exopthalmos***
May precipitate thyroid storm so pretreat with thionamide
Term
Potassium iodide
Definition
Inhibit release of preformed T3 and T4 via competitive antagonist for iodine uptake.
Used to treat thyroid storm and to prepare hyperthyroid for surgery.
Not for long term.
SE - sore throat, ulcers, rashes, metallic taste
Term
Methimazole
Definition
a thionamide (TH synthesis inhibitor)
Oral. Inhibits TPO
minimal effect on exophthalmos
No effect on release of preformed TH
less frequent dosing compared to PTU due to longer half life
Hypersensitivity reaction (increase wbc), rash, arthralgia, fever, edema
allergic to this or PTU. not both
Preferred in the treatment of graves due to decreased toxicity
Term
Propylthiouracil
Definition
Oral. a thionamide (TH synthesis inhibitor)
Inhibits TPO, in addition blocks T4 ->T3 conversion. (thus is preferred in thyroid storm). Preferred in pregnancy
Has no effects on release of preformed TH
minimal effect on exophthalmos
Hypersensitivity rxn, and flu like sxs.
Hepatitis black box warning. Flu like symptoms. allergic to this or methimazole. not both
Term
Testosterone Enanthate
Definition
highly lipophillic. given via injection
Term
Testosterone cypionate
Definition
Highly lipophillic and given via injection. depo-testosterone
Term
Oxandrolone
Definition
17a-alyklated testosterone. good for oral absorption but causes hepatotoxicity.
Term
Gosarelin
Definition
GnRH analog. desensitizes the GnRH signaling pathway via decreasing LH and FSH secretion and testosterone production
Term
Nafarelin
Definition
GnRH analog. Desinsitizes GnRH pathway via inhibition of LH and FSH and testosterone production.
Term
Ganirelix
Definition
GnRH competitive antagonist for GnRH receptors in anterior pituitary
Term
Cetrorelix
Definition
GnRH competitive antagonist for GnRH receptors in anterior pituitary
Term
Flutamide
Definition
Androgen Receptor Antagonist. Used to treat prostate cancer combined w/ GnRH analogs. also used to treat hirsutism in women
also used to treat congenital adrenal hyperplasia b/c steroid synthesis is shifted to androgens.
SE - hepatotoxicity
Term
Bicalutamide
Definition
Androgen Receptor Antagonist
Used in prostate cancer and w/ GnRH analogs
Term
Spironolactone
Definition
it is mostly a mineralocorticoid w/ weak anti-androgenic effects.
Treats cushings and hyperaldosteronism
SE - gynecomastia
Term
Finasteride
Definition
5a-reductase inhibitor. Thus blocks DHT formation -> BPH symptom relief.
Blocks mainly Type II reductase
SE - impotence, decreased libido, and gynecomastia
Term
Dutasteride
Definition
5a-reductase inhibitor. used to reduce DHT formation and treat BPH.
Inhibits type 1 and 2 reductase.
SE - impotence, decreased libido, and gynecomastia.
Term
Terazosin
Definition
alpha 1 blocker. relaxes smooth muscle around prostate, urethra, and neck of bladder.
First line in BPH pts.
SE - decreased ejaculation
Term
Doxazosin
Definition
alpha 1 blocker. Relaxes prostate, urethra, and neck of bladder.
First line treatment for BPH.
SE - decreased ejaculation
Term
Tamsulosin
Definition
alpha 1 blocker. Relaxes smooth muscle around prostate, urethra, and neck of bladder.
SE - decreased ejaculation and prolonged QT interval.
Term
Rapid acting insulin
Definition
takes effect in 15-30 min and lasts 3-5 hours. They are modified for rapid absorption and dissolution into monomers
Term
Short acting insulin
Definition
identical to human insulin. Peaks in 2-3 hours, lasts 5-8 hours.
Forms dimers and hexamers. Take before meals due to slower absorption rates.
Term
Glargine
Definition
long lasting peakless insulin.
Soluble in acidic pH and precipitates in neutral pH of subQ tissue. Then slowly dissolves.
Do not mix w/ other insulin preparations
Term
Detemir
Definition
further modified insulin giving it long term affects via increased albumin binding and self-aggregation.
Term
Glipizide
Definition
sulfonylureas - cause a hypoglycemic effect by stimulating the release of insulin. MOA: bind to SUR1 K channel and cause depolarization.
Uses - type 2 diabetics.
CI - Type 1 DM, pregnant, hepatic/renal insufficiency
SE - hypoglycemia, N/V, aplastic/hemolytic anemia, B-cell burnout, weight gain, sulfa allergy
Displaced by sulfonamides, clofibrate and salicylates.
Term
Glimepiride
Definition
sulfonylureas - cause a hypoglycemic effect by stimulating the release of insulin. MOA: bind to SUR1 K channel and cause depolarization.
Uses - type 2 diabetics.
CI - Type 1 DM, pregnant, hepatic/renal insufficiency
SE - hypoglycemia, N/V, aplastic/hemolytic anemia, B-cell burnout, weight gain, sulfa allergy
Displaced by sulfonamides, clofibrate and salicylates.
Term
NPH
Definition
intermediate acting insulin. Onset 2-5 hours and lasts 4-12 hours.
Usually mixed w/ rapid or short acting.
Term
Repaglinide
Definition
cause hypoglycemia via increase release of insulin via closing K channel.
Absorbed rapidly. Can be used w/ insulin sensitizers, but not sulfonylureas
Less effective at reducing A1c than SUs.
Term
Metformin
Definition
Insulin sensitizer. First line drug in Type II DM.
anti-hyperglycemic action via activation of AMP dependent kinase -> increase insulin action in muscle and fat.
SE - anemia (B12 absorption), N/V, abd pain, flatulence, Lactic acidosis.
CI - hepatic/renal insufficiency
Term
Pioglitazone
Definition
agonist for PPAR-y -> activates insulin responsive genes causing increased insulin sensitivity.
SE - liver function monitoring, anemia, weight gain, edema, volume expansion, increased fracture risk
CI - nursing mothers.
Term
Acarbose
Definition
a-glucosidase inhibitor. competitively inhibits enzymes in glucose metabolism in the gut. Slow absorption.
SE - malabsorption, flatulence, diarrhea, abd bloating
Term
Miglitol
Definition
a-glucosidase inhibitor. inhibits carbohydrate metabolism in gut.
SE - reduce dose if creatinine < 30, malabsorption, diarrhea, flatulence, abd bloating.
Term
Pramlinitide
Definition
amylin analog. Delays gastric emptying, inhibits glucagon secretion, and synergistic w/ insulin
SE - hypoglycemia, GI (N/V, anorexia)
Term
Exanatide
Definition
GLP-1 analog that stimulates the Gs GLP-1 receptor increasing insulin gene expression and beta cell mass.
Actions are glucose dependent -> dose not cause hypoglycemia.
Also an incretin mimetic.
DPP-IV resistant
SE - N/V, hypoglycemia w/ insulin or secretagogues, weight loss, no B-cell burnout
Term
Liraglutide
Definition
GLP-1 analog.
interacts w/ albumin -> increase T1/2 -> once daily dosing.
SE - N/V, hypoglycemia w/ insulin or secretagogues, weight loss, no B-cell burnout
Term
Sitagliptin
Definition
DPP-IV inhibitor converted to active metabolite by CYP3A4. excreted unchanged in urine -> reduce in kidney pts.
SE - no GI, and mild hypoglycemia
Term
Desmopressin
Definition
a synthetic vasopressin that mainly activates the V2 receptors in the kidney to increase water reabsorption.
abdominal cramping.
used for nocturnal enuresis.
Term
Drugs that cause hyperthyroidism
Definition
Iodides, Amiodarone, and Lithium.
Term
Propanolol
Definition
beta blocker that prevents the sympathetic activation of adrenergic receptors.
also, inhibits 5-deiodinase in peripheral tissue. (The only beta blocker that does this)
Term
Prochlorperazine
Definition
1st generation antihistamine that is an Anti-emetic. blocks dopamine receptors.
antagonizes chemotherapy effects but limited b/c of sedation and extrapyramidal effects.
Sedation side effect makes it useful for vomiting pts who can't sleep.
Term
ondansetron
Definition
5HT inhibitor. blocks serotonin in CTZ.
Most efficacious for chemo/radiation/pregnancy emesis. better than metoclopramide.
Dosage needs to be adjusted for hepatic insufficient pts.
Term
Metoclopramide
Definition
central dopamine antagonist as well as increases LES pressure. Elevates the CTZ threshold.
Indicated for diabetic gastroperesis and chemo emesis.
Avoid high doses for extrapyramidal effects -> induce parkinson symptoms**
Term
Diphenhydramine
Definition
h1 antihistamine. don't worry
It's fucking Benadryl.
Term
Meclizine/Hyoscine
Definition
H1 antihistamines that also has anti-muscarinic effects. prevents motion sickness. But limited by sedation, and anti-muscarinc effects (dry mouth, urinary retention)
Term
Diphenoxylate
Definition
opiod anti-diarrheal.
inhibits mucosal peristaltic reflex.
Metabolized to active metabolite.
Peripheral and CNS effects. Give to travelers with diarrhea who can't sleep
Formulated w/ atropine to prevent abuse
Term
Loperamide (imodium)
Definition
Opiod anti-diarrheal. Inhibits GI peristalsis
Indicated for non-specific diarrhea and IBD.
Used if you need to go to work b/c no CNS effects.
Term
Sulfasalazine
Definition
An aminosalicylate. Releases 5-aminosalicylic acid (anti-inflammatory) and sulfaperidine (anti-bacterial) in large intestine. First step to treat IBD
Term
bismuth subsalicylate
Definition
AKA Pepto-Bismol
hydrolyzed to salicylate. anti-secretory, anti-inflammatory, and anti-baterial effects. inhibits prostaglandins to reduce hypermotility and inflammation.
cytoprotective adjunct agent used in Peptic Ulcer disease and used to treat diarrhea
Term
Olsalazine
Definition
An aminosalicylate. Releases 5-aminosalicylic acid in large intestine
Treats IBD
Term
Balsalzide
Definition
An aminosalicylate. Releases 5-aminosalicylic acid in large intestine
Treats IBD
Term
Mesalamine compounds (4)
Definition
pentasa, Asacol, Rowasa, and Canasa
used if pts not responding to aminosalicylates
Has an asa in the name
decreases leukotrienes and scavenges free radicals
Term
Methotrexate
Definition
immunosuppressant that suppresses DHF reductase and production of tetrahydrofolate used in purine/prymidine synthesis. Used to treat IBD by reducing proliferation of inflammatory cells in the GI.
Term
Infliximab
Definition
TNF-a antagonist.
Used in severe crohns disease.
don't confuse w/ abciximab (IIb/IIIa inhibitor)
Term
Name 2 anti-spasmotic agents used to treat IBS.
Definition
Scopolamine and dicyclomine
Term
Name an TCA used to treat IBS
Definition
Amitryptiline or doxeprin
Term
Ulcerative Colitis
cytokines? involved bowel?
Definition
IL-1, IL-6, and TNF.
colon and rectum are infiltrated w/ immune cells
Term
Name 3 SSRI's that are used to treat IBS and how they work
Definition
Fluoxetine, sertraline, and paroxetine.
modulation of pain via preventing serotonin reuptake in the synapse. Very effective.
Term
What is the order of treatment for IBD?
Definition
aminosalycylates (sulfasalazine) or mesalamines (pentasa, asacol, rowasa)
Corticosteroids
Immunosuppressive agents (methotrexate, azathioprine, and 6-mercaptopurine)
Monoclonal antibodies (infliximab)
Surgery (indicated if fistulas, adhesions, and obstructions
Term
Dicyclomine
Definition
Anti-sposmotic agent that treats symptoms of IBS
Term
Cimetidine
Definition
An H2 receptor antagonist. Blocks acid secretion by the parietal cells in stomach to treat GERD decreases hepatic metabolism of warfarin, phenobarbital, phenytoin, diazepam, and propanolol because it is a potent inhibitor of the cytp450 system
Term
Misoprostol
Definition
stimulates Gi coupled prostaglandin receptor on stomach parietal cell to treat GERD
Not used in cardiac patients
Term
exomeprazole
Uses? side effects?
Definition
used in Peptic ulcer disease and GERD.
Inhibits p450 -> decreased elimination of phenytoin, diazepam, and warfarin.
Term
Omeprazole
Definition
Direct irreversible PPI, Most effective in treating GERD and PPI. its a prodrug. converted in parietal cell to active form.
Inhibits 3A4 -> buildup of phenytoin, diazepam, and warfarin
fast onset.
Term
How do you diagnose H. Pylori infection
Definition
MC is urea breath test b/c pylori is urease positive.
can also do endoscopy, and serology
Term
Antacid side effects?
Definition
systemic alkalosis
diarrhea
magnesium antacids should be avoided in pts w/ renal impairment
Interferes w/ digoxin, ketoconazole, and INH absorption.
Term
Ranitidine (Zantac)
Definition
anti-ulcer drug. binds and inhibits H2 receptor. H2 receptor blocker. Doesn't mess w/ CytP450 system.
Term
A pt is on phenytoin, a drug metabolized by the p45o system, and develops a peptic ulcer, which PPI is preferred?
Definition
Rabeprazole
Term
lansoprazole
Definition
PPI aka prevacid. FDA approved for infants
PPI.
May interfere w/ absorption of digoxin, ketoconazole and isoniazid
Term
Esomeprazole
Definition
PPI. aka nexium.
May interfere w/ absorption of digoxin, ketoconazole and isoniazid.
Inhibits 3A4 -> buildup of phenytoin, diazepam, and warfarin
Term
What is the first line therapy three drug protocol for H. Pylori induced peptic ulcer?
Definition
omeprazole
clarithromycin
amoxicillin/metronidazole
Term
mifepristone**
Definition
Treats Cushings via antagonist at glucocorticoid receptor (no effect on cortisol)
Used for hyperglycemia from hypercortisolism and for pts failed surgery or not surgery candidates.
SE - endometrial proliferation and vaginal bleeding b/c progesterone receptor antagonist. (Estrogen goes cray)
CI - pregnancy, C3A4 drugs (statins, corticosteroid therapy, women w/ endometrial issues.
QT prolongation, hypokalemia, and hypocortisolism.
Term
ketoconazole
Definition
inhibits gonadal and adrenal steroid hormone release.
Unlabeled use in cushings.
SE - hypersensitivity and GI disturbance
Term
Metyrapone
Definition
inhibits 11b-hydroxylase -> increased 11 deoxycorticosteroids and androgens.
Treats ectopic ACTH syndrome, and used for pregnant women w/ cushings.
SE - salt/water retention, hirsutism, transient dizziness
Term
Aminoglutethimide
Definition
inhibits conversion of CH -> pregnenolone.
Treats - cushings from adrenal carcinoma, ACTH producing tumors, adrenal hyperplasia.
SE - lethargy, drowsiness, headache, N/V
Term
Spironolactone (adrenal use)
Definition
antagonist of mineralocorticoid receptor and androgen receptors.
SE-gynecomastia
Term
Pasireotide
Definition
agonist at somatastatin receptor 5. Inhibits ACTH release.
treats adults w/ cushings who can't have surgery.
SE - hypocortisolism (lower dose), hyperglycemia and DM (significant via inhibition of insulin), QT prolongation, cholelithiasis (just like octreotide)
Term
cosyntropin
Definition
synthetic ACTH. Used to detect addisons.
Term
anastrazole
Definition
aromatase inhibitor. Used in treatment of congenital adrenal hyperplasia and endometriosis
Term
letrazole
Definition
aromatase inhibitor. Used in treatment of congenital adrenal hyperplasia and endometriosis
Term
Glucagon-like peptide 1
Definition
increase glucose dependent insulin secretion, decrease glucagon secretion, decrease appetite.
This is a good molecule to have in diabetes.
Degraded by dipeptidal peptidase IV (DPP-IV)
Term
Chrohns Disease
cytokines? Bowel involved? Sxs and signs?
Definition
IL-1,6, and 12. TNF and IFN-a.
macrophages, neutrophils and leukocytes infiltrate.
Affects the entire GI tract.
abd tenderness, frequency, bloody stool, low fever, high CRP.
Term
Orthoevra
Definition
combination patch. High risk of DVT.
Term
Nuvaring
Definition
a combination contraceptive. Ethinyl estradiol/etonogestrel. Less effective than the pill
Term
Etonorgestrel
Definition
The hormone contained in the progestin implants and in nuvaring. Cheap. Lasts for years. Fertility rapidly returns.
Term
Depot-medroxyprogesterone acetate
Definition
a long acting progestin only contraceptive. IM injection every three months. almost 100% effective. Infertility persists after discontinuation
Term
Drosperinone (Yasmin)
Definition
Progesterone w/ mineralocortocoid antagonistic action. Causes increase in serum K in pts that are on ACEs or K sparing diuretics.
Term
Postcoital contraception
Definition
contain a high dose of progesterone to prevent the implantation of the possibly fertilized egg.
Term
Ethinyl Estradiol
Definition
the typical estrogen component of birth control.
Term
Conjugated equine estrogens
Definition
Used for HRT. has a short acting estrogen mixture of conjugated estrogens in order to successfully get by first pass metabolism
Used in women who have had a hysterectomy
Term
Esterified estrogens
Definition
Synthetic estrogens used for HRT. hydrolyzed by the gut enzymes to get across the membrane
Term
Clonidine
Definition
specifically used to treat the hot flashes in menopause via central a2 agonist
Term
Desvenlafaxine
Definition
SSRI used to treat hot flashes in menopause
Term
what drugs when administered with contraceptives will induce contraceptive failure
Definition
drugs that induce p450 metabolism such as rifampin, carbamezepine, and phenytoin
Term
Leuprolide
Definition
a GnRH analog used to suppress gonadotropin secretion and eliminate estrogen production to treat endometriosis.
Term
physiological actions of progestins
Definition
increase adipose tissue via inhibition of hormone sensitive lipase. Natriuretic peptide, elevates body temp, promotes healthy skin, increase insulin sensitivity. Raises the LDL and decreases the HDL
Term
adrogenic effects of progestins excess? Name 5
Definition
increased appetite, weight gain, tired/fatigue, acne, oily scalp, hair loss, hirsuitism, breast regression, depression, yeast infections
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