Term
|
Definition
Ultra-short-acting synthetic insulin prep
Alteration of amino acid sequences to decrease hexamer stability (monomer form is the active form)
Reach peak concentration in blood quickly-> take right before a meal
Clear solutions w/ neutral pH; small amount of Zn for stability |
|
|
Term
|
Definition
aka Humulin
Short-acting (rapid) insulin prep
Regular insulin hexamer in clear solution w/ neutral pH; small amount of Zn for stability |
|
|
Term
|
Definition
Intermediate-acting insulin prep
Protamine (insulin binding protein) combined w/ insulin in phosphate buffer-> IBP allows slower insulin release
Often used as mixed injection w/ regular insulin (70% NPH, 30% regular insulin)-> allows both rapid and imm effects |
|
|
Term
|
Definition
Intermediate-acting insulin prep
Precipitate of insulin w/ Zn in acetate buffer-> Zn increases hexamer stability
Cannot use as a premixed injection w/ regular insulin-> Zn stabilizes regular insulin into an imm form |
|
|
Term
|
Definition
Long (slow) acting insulin prep
High Zn concentration in acetate buffer-> slow acting w/ unpredictable absorption |
|
|
Term
|
Definition
Long (slow) acting insulin prep
Amino acid substitutions allow increased hexamer stability w/ prolonged and predictable absorption from subcutaneous injection
Clear solution w/ pH 4 |
|
|
Term
|
Definition
Long (slow) acting insulin prep
Attachment of fatty acid to amino acid allows increased hexamer formation and increased albumin binding |
|
|
Term
|
Definition
Oral Type II Diabetes Agents
MOA: close ATP sensitive K+ channels to promote insulin release; may also directly promote exocytosis
SE: hypoglycemia and weight gain w/ all, alcohol-induced flushing and hyponatremia w/ chlorpropamide (secondary to increase in ADH's effect on kidney)
1st gen: tolbutamide, chlorpromide (long half-life), tolazamide, acetohexamide
2nd gen: glyburide, glipizide, gliclazide, glimepiride
-> more potent; short half-life w/ similar duration of action to 1st gen. |
|
|
Term
|
Definition
Meglitinides- oral type II DM agents
MOA: close ATP sensitive K+ channels to promote insulin release w/o directly effecting exocytosis
Lack sulfur (used for pts w/ sulfur allergies)
Duration of action: repaglinide > nateglinide |
|
|
Term
|
Definition
Biguanide- oral type II DM agent
MOA: increases peripheral effects of insulin via increased AMP kinase activation and decreases hepatic and renal glucose output
Not a hypoglycemic and does not increase insulin release
SE: GI symptoms, lactic acidosis
C/I: renal impairment, hepatic disease, history of lactic acidosis |
|
|
Term
Rosiglitazone
Pioglitazone |
|
Definition
Thiazolidinediones-oral type II DM agents
MOA: binds to PPAR(gamma) to increase transcription of glucose transporters (GLUT4)-> increases effects of insulin (reduces insulin resistance)
SE: both- fluid retention/edema=> risk of heart failure; rosiglitazine- increased risk of infarcts; pioglitazone- increased risk of bladder cancer |
|
|
Term
|
Definition
Oral type II DM agents
MOA: alpha-glucosidase inhibitors-> decrease GI carb absorption
SE: flatulence, diarrhea, abdominal pain |
|
|
Term
|
Definition
Oral type II DM agent
MOA: inhibits dipeptidyl peptidase (DPP-4)-> prevents degradation of incretins (hormones that increase insulin release- like GLP-1)
Increases glucose mediated insulin release, lowers glucagon levels, slows gastric emptying, decreases appetite
SE: rhinitis, upper respiratory infections, allergic reactions |
|
|
Term
|
Definition
Type II DM agent
MOA: glucagon like peptide (GLP-1) analog-> increases glucagon dependent insulin secretion
Increases glucose mediated insulin release, lowers glucagon levels, slows gastric emptying, decreases appetite
Given parenterally
SE: nausea, headache, vomiting, mild weight loss, pancreatitis |
|
|
Term
|
Definition
Amylin analog- type II DM agent
MOA: binds amylin receptor-> modulates postprandial glucose levels, suppresses glucagon release, delays gastric emptying, anorectic effects (decreases appetite)
Given as preprandial subcutaneous injection
SE: nausea, anorexia, hypoglycemia, headache |
|
|
Term
|
Definition
Hyperglycemic
Synthesized in pancreatic alpha-cells
Effects: hepatic glycogenolysis, gluconeogenesis, and ketogenesis (no effect on muscle glycogen); inotropic and chronotropic effects; intestinal smooth muscle relaxation
USE: severe hypoglycemia, endocrine diagnosis, beta-blocker overdose (to reverse cardio effects), bowel radiology (b/c it relaxes the intestine)
Given parenterally
SE: transient nausea/vomiting |
|
|
Term
|
Definition
Hyperglycemic
MOA: prevents closure of ATP regulated K+ channels to prevent insulin release
Opposite of sulfonylureas |
|
|
Term
|
Definition
Anti-diuretic hormone (ADH)
MOA: V1 receptor on vascular smooth muscle-> increase BP; V2 receptor on renal collecting duct principal cells-> water retention and increase BP
Released from posterior pituitary |
|
|
Term
|
Definition
Vasopressin synthetic analog
MOA: selective V2 agonist-> promote fluid retention
Tx of central diabetes insipidus |
|
|
Term
| Treatment: Central Diabetes Insipidus |
|
Definition
Desmopressin
Chlorpropamide-sulfonylurea (increases ADH effect downstream of receptor)
Carbamazapine and Clofibrate- increase ADH effect |
|
|
Term
| Treatment: Nephrogenic Diabetes Insipidus |
|
Definition
Thiazide diuretics
Indomethacin- increases ADH effects by clocking PGs
Amiloride (for Li induced DI)- Li interferes w/ V2 signaling pathway, amiloride blocks Li uptake |
|
|
Term
|
Definition
Water restriction, Hypertonic saline
Demeclocycline- interferes w/ V2 pathway
Loop diuretics
Lithium
Conivaptan- ADH receptor antagonist |
|
|
Term
|
Definition
Synthetic = Pitocin
Released from posterior pituitary
Effects: stimulates uterine contraction (induce labor) and milk ejection from mammary glands |
|
|
Term
Misoprostol
Carboprost
Dinoprostone |
|
Definition
Prostaglandin analogs
Misoprostil- PGE1
Carboprost- PGF2alpha
Dinoprostone- PGE2
Tx: postpartum hemorrhage, therapeutic abortion -> stimulate uterine contraction |
|
|
Term
Ergonovine
Methylergonovine |
|
Definition
Ergot analogs
Tx: postpartum hemorrhage-> stimulate uterine contraction |
|
|
Term
|
Definition
Tocolytic agents- uterine relaxants
MOA: β2-adrenergic agonists-> relax smooth muscle
SE: increase renin release (some beta1 action), hypokalemia, pulmonary edema, skeletal muscle tremor, anxiety, hyperglycemia
Use: delay labor |
|
|
Term
|
Definition
Tocolytic agents- uterine relaxants
MOA: Ca+2 channel blockers-> relax smooth muscle
Use: delay labor |
|
|
Term
|
Definition
Tocolytic agents- uterine relaxants
MOA: prostaglandin-synthetase inhibitor-> decrease prostaglandins
Tx of nephrogenic diabetes insipidus (increases ADH effects in kidney), delay labor
SE: premature closure of ductus arteriosus |
|
|
Term
|
Definition
Tocolytic agents- uterine relaxants
MOA: oxytocin receptor antagonist-> prevents uterine contraction
Use: delay labor |
|
|
Term
|
Definition
|
|
Term
|
Definition
Recombinant IGF-1 analog w/ binding protein
Tx of GH resistance (i.e. Laron dwarfism) |
|
|
Term
|
Definition
GHRH analog
Diagnostic agent w/ some therapeutic use |
|
|
Term
|
Definition
GH receptor antagonist
Tx of pituitary adenoma (somatotroph) |
|
|
Term
|
Definition
Somatostatin analogs
MOA: inhibit GH and TSH release
Tx of pituitary adenomas (somatotroph, thryrotroph)
Compared to somatostatin, longer half-life and more pituitary action w/ less GI and pancreas activity |
|
|
Term
Levothyroxine (Synthroid)
Liothyronine
Liotrix |
|
Definition
Synthetic thyroid hormones
Levothyroxine- T4
Liothyronine- T3
Liotrix- T4 and T3
T4 analog used mostly, allows T4-> T3 conversion for maximal normal regulation
Tx of hypothyroidism, cretinism, TSH suppression in thyroid cancer
SE: hyperthyroidism, cardiac arrhythmia |
|
|
Term
Propylthiouracil (PTU)
Methimazole |
|
Definition
Antithyroids
MOA: inhibits thyroid peroxidase oxidation of iodide and inhibits coupling reaction (DIT and MIT); PTU also inhibits peripheral deiodination of T4 to T3 (type I 5'-deiodinase)
Half-life: methimazole > PTU
SE: hypothyroidism, rash, agranulocytosis w/ sore throat and fever |
|
|
Term
Thiocyanate
Perchlorate
Fluroborate |
|
Definition
Ionic inhibitors
MOA: interfere w/ iodide concentration-> compete for I- uptake in thyroid at Na/I symport
SE: fatal aplastic anemia (perchlorate) |
|
|
Term
|
Definition
Anti-thyroid
MOA: interferes w/ release of T3 and T4
Use: cause hypothyroidism |
|
|
Term
| Iodide and iodine-containing drugs |
|
Definition
Wolff-Chaikoff effect-> reduction in thyroid hormone levels caused by ingestion of a large amount of iodide (toxic I- levels decrease thyroid hormone production)
Rapid effect (1-3 days) followed by escape phenomenon-> decrease number of Na-I symporters to decrease I- transport in thyroid=> allows recovery of TH production
Ex: amiodarone, Lugol's solution (KI), radiology contrast reagents
Use: preoperative treatment for thyroidectomy; thyrotoxic crisis |
|
|
Term
|
Definition
Destroys tissue into which it is taken up (thyroid gland)
127-I = stable isotope
131-I = half-life 8days, therapeutic use
123-I = half-life 13hrs, diagnostic use
131-1: Tx of metastatic thyroid carcinoma along w/ TSH to enhance uptake
Used more in older pts, not indicated in pregnancy
SE: hypothyroisism |
|
|
Term
|
Definition
IV- Ca chloride, Ca gluconate, Ca gluceptate
Oral- Ca carbonate, Ca citrate, Ca lactate
Treatment of osteoporosis, hypocalcemia |
|
|
Term
Cholecalciferol
Ergocalciferol |
|
Definition
|
|
Term
|
Definition
Vitamin D analog of 25-hydroxycholecalciferol
Treatment of osteoporosis, hypocalcemia, hypoparathyroidism, nutritional deficiency
Used in patients w/ hepatic disease (doesn't require hepatic 25-hydroxylation) |
|
|
Term
|
Definition
Vitamin D analog of 1,25-dihydroxycholecalciferol
Treatment of osteoporosis, hypocalcemia, hypoparathyroidism, nutritional deficiency
Used in patients w/ renal disease (doesn't require hepatic 25-hydroxylation or renal 1-hydroxylation)
Calcipotriol- less potent, main use in psoriasis (pro-differentiation) |
|
|
Term
|
Definition
Vitamin D synthetic derivative
Treatment of osteoporosis, hypocalcemia, hypoparathyroidism, nutritional deficiency
Does not require 1-OH for activation but does require 25-OH in liver
Able to use in patients w/ renal disease |
|
|
Term
Doxercalciferol (1-hydroxyvitamin D2)
Alfacalcidol (1alpha-Hydroxycholecalciferol) |
|
Definition
Vitamin D synthetic derivative
Treatment of osteoporosis, hypocalcemia, hypoparathyroidism, nutritional deficiency
Already contains the 1-OH but requires 25-OH in liver
Able to use in patients w/ renal disease |
|
|
Term
|
Definition
Calcitriol analog
Reduces PTH w/o hypercalcemia
Used in chronic renal failure; little GI action |
|
|
Term
|
Definition
Calcitriol analog
MOA: suppressor of PTH gene expression
Limited action on intestine and bone; used in chronic renal failure w/ secondary hyperparathyroidism or in primary hyperparathyroidism
Low affinity for serum binding protein leads to longer half-life than calcitriol |
|
|
Term
|
Definition
Treatment of osteoporosis, hypercalcemia
MOA: prevents Ca2+ absorption in the intestines, decrease Ca2+ and phosphate reabsorption in kidney, and prevents reabsorption in bone-> direct effect on osteoclasts
Salmon and synthetic human forms-> salmon more potent
Given parenterally |
|
|
Term
|
Definition
MOA: act on osteoblasts to decrease osteoclast recruitment and activation-> promote osteoprotegrin (decoy receptor) synthesis in osteoblasts=> binds osteoclast differentiation factor (aka RANK) to prevent osteoclast activation
Tx: osteoporosis |
|
|
Term
|
Definition
PTH analog
MOA: intermittent administration promotes bone growth
Often combined w/ a bisphosphonate (alendronate) |
|
|
Term
| Corticosteroids (glucocorticoids)-> Ca2+ effects |
|
Definition
| MOA: antagonize VitaminD stimulated GI Ca2+ absorption, stimulate renal Ca2+ excretion, block bone collagen synthesis, and increase PTH stimulated bone reabsorption |
|
|
Term
|
Definition
Treatment of osteoporosis, hypercalcemia
MOA: very similar in structure to pyrophosphate, but contains P-C bonds, which osteoclasts cannot break down; when taken up by osteoclasts, slows formation of hydroxyapatite crystals and decreases osteoclasts function
Side effect: GI irritation |
|
|
Term
Etidronate
Pamidronate
Alendronate
Risedronate
Tiludronate
Zoledronate
Ibandronate |
|
Definition
Bisphosphonates
Etidronate and Tiludronate-> also metabolized into an ATP analog that accumulates in osteoclast and induces apoptosis
Etidronate-> Side effect: osteomalacia, NO GI irritation
Alendronate-> also inhibits protein prenylation in osteoclasts=-> decreased function; less of a side effect of decreased bone mineralization compared to the others
Zoledronate-> renal toxicity |
|
|
Term
|
Definition
Calcimimetic
MOA: inhibits PTH secretion by lowering the concentration of Ca2+ at which PTH secretion is suppressed-> increases sensitivity
Use: treatment of primary and secondary hyperparathyroidism and hypercalcemia associated with parathyroid carcinoma |
|
|
Term
|
Definition
Treatment of hypercalcemia; Paget's disease
MOA: cytotoxic antibiotic that also decreases plasma Ca2+ concentrations by inhibiting bone resorption
Toxicity: thrombocytopenia |
|
|
Term
|
Definition
Oral agent
MOA: binds free ionized Ca2+
High risk procedure |
|
|
Term
|
Definition
Reduces renal Ca excretion
Use: inhibits renal Ca stone formation; treatment of osteoporosis; Tx of nephrogenic diabetes insipidus (unknown MOA) |
|
|
Term
|
Definition
Accumulates in bone and teeth
MOA: may stabilize hydroxyapatite-> increases bone volume; may increase osteoblast activity
Both acute and chronic toxicities limit use |
|
|
Term
|
Definition
ACTH analog
Diagnostic use to test adrenal response |
|
|
Term
|
Definition
Adrenocorticosteroid
Anti-inflammatory and immunosuppressive
MOA: ↓ arachidonic acid metabolism (both PGs and LTs)-> ↓ COX-2 mRNA and protein and ↓ PLA2 activity; ↓ cytokine expression (esp ILs); ↓ cell-adhesion molecule expression (traps neutrophils in vascular compartment); ↓ fibroblast DNA synthesis/proliferation
Adverse effects: adrenal suppression, fluid and electrolyte abnormalities, metabolic changes, edema, hypertension, osteoporosis, growth suppression in children, cataracts, behavioral changes
Must taper off; do not abruptly stop-> adrenal glands begin to shut down so you have to allow them to start back up
Use: replacement therapy, CAH, asthma, etc. |
|
|
Term
|
Definition
Cortisol- naturally occurring; hydrocortisone- synthetic
Short to medium acting glucocorticoid; half life 60-90mins
Oral, injectable, topical; production governed by ACTH
Increased w/ stress, hypothyroidism, and liver disease
Greatest metabolism in liver; 20% by 11-beta-hydroxysteroid dehydrogenase 2 in kidney (inactivated to cortisone)-> 11beta-HSD2 inhibited by licorice
Cortisone activated to cortisol in liver-> 11-beta-HSD1 |
|
|
Term
Prednisone
Methylprednisolone
Prednisolone |
|
Definition
Glucocorticoid
Prednisone is a prodrug that must be activated in the liver to prednisolone (synthetic = methylprednisolone)
4X stronger anti-inflammatory than cortisol and causes less Na+ retention in the kidneys
Intermediate duration of action
SE: glucose intolerance, immunosuppresion, osteoporosis, psychosis |
|
|
Term
|
Definition
Intermediate acting glucocorticoid
5X stronger anti-inflammatory than cortisol w/ no MR potency |
|
|
Term
Betamethasone
Dexamethasone |
|
Definition
Long acting glucocorticoids
25X stronger anti-inflammatory than cortisol w/ no MR potency
Induces a strong ACTH suppression-> "Dexamethasone suppression test" |
|
|
Term
|
Definition
Glucocorticoid
10X stronger anti-inflammatory than cortisol but causes 125X more Na+ retention in the kidneys
Short duration of action
Used in patients w/ hypoaldosteronism |
|
|
Term
|
Definition
Anti-adrenocorticosteroid; anti-progestin
MOA: glucocorticoid and progestin receptor antagonist
Tx of cortisol excess |
|
|
Term
|
Definition
Anti-adrenocorticosteroid
MOA: adrenal lytic agent-> decreases corticosteroid biosynthesis |
|
|
Term
|
Definition
Anti-adrenocorticosteroid
MOA: inhibits P450scc (side chain cleavage enzyme) and also P45011beta (11beta-hydroxylase) and aromatase
Decreased cortisol, aldosterone, and sex steroids
Tx: hyper-hormone states, breast cancer |
|
|
Term
|
Definition
Anti-adrenocorticosteroid
MOA: inhibits P45017alpha (17,20-lyase); also inhibits P450scc at high doses
Decreases sex-steroid biosynthesis |
|
|
Term
|
Definition
Anti-adrenocorticosteroid
MOA: inhibits 3beta-hydroxysteroid dehydrogenase (3beta-HSD)
Decrease adrenocorticoid biosynthesis |
|
|
Term
|
Definition
Anti-adrenocorticosteroid
MOA: inhibits P45011beta (11beta-hydroxylase)
Decrease aldosterone and cortisol biosynthesis, increased androgen biosynthesis |
|
|
Term
|
Definition
GnRH analog- short-acting
Given in pulsatile form IV to stimulate LH/FSH release |
|
|
Term
Leuprolide
Histrelin
Nafarelin
Goserelin
Buserelin
Deslorelin
Triptorelin |
|
Definition
GnRH analogs- long-acting
MOA: continuous administration w/ initial stimulation of LH/FSH production followed by LH/FSH suppression after 2 weeks via GnRH receptor downregulation
Use: adjunct to fertility treatment, treatment of precocious puberty, chemical castration, prostate/breast cancer |
|
|
Term
Ganirelix
Cetrorelix
Abarelix |
|
Definition
GnRH antagonists- long-acting
Decrease LH/FSH production
Use: adjunct to fertility treatment, treatment of precocious puberty, chemical castration, prostate/breast cancer |
|
|
Term
| Human Chorionic Gonadotropin (hCG) |
|
Definition
|
|
Term
Menotropins
Urofollitropin
Follitropin |
|
Definition
LH/FSH analogs
Menotropins- both LH and FSH
Urofollitropin- FSH >> LH
Follitropin- recombinant FSH |
|
|
Term
| Parenteral Testosterone Ester Preparations |
|
Definition
Esterified testosterones-> increased lipid solubility
Testosterone propionate- short acting (2-3X/wk)
Testosterone cypionate/enanthate- long acting (once every 2-3wks)
Parenteral administration
Use: primary hypogonadism, improves N balance
SE: virilization, anemia, osteoporosis, breast cancer |
|
|
Term
Danazol
Stanozolol
Fluoxymesterone
Methyltestosterone
Oxandrolone |
|
Definition
17α-alkylated androgens-> decreased hepatic metabolism, increased oral bioavailability, and increased hepatic toxicity
Tx: hereditary angioneurotic edema, androgen therapy |
|
|
Term
|
Definition
Anti-adrenocorticosteroid; Anti-androgen
MOA: mineralocorticoid receptor (MR) aka aldosterone receptor antagonist; also inhibits androgen synthesis-> 17-alpha-hydroxylase inhibitor (use in prostate cancer)
Tx of hyperaldosteronism, HTN, hirsutism
Toxicity: cross rxn w/ androgen receptor (gynecomastia, impotence)-> less w/ eplerenone |
|
|
Term
|
Definition
Anti-androgen
MOA: inhibits 5α-reductase (type II > type I)-> prevents conversion of testosterone to dihydrotestosterone
Tx: BPH, male pattern baldness (type II reductase) |
|
|
Term
|
Definition
Anti-androgen
MOA: 5alpha-reductase inhibitor (type II = type I)-> decreases DHT action |
|
|
Term
|
Definition
Anti-androgen
MOA: steroidal androgen receptor antagonist; progesterone receptor agonist-> decreases LH/FSH
Rarely used alone; used in combo w/ GnRH agonist during first few weeks of treatment to prevent excess androgen production |
|
|
Term
Flutamide
Bicalutamide
Nilutamide |
|
Definition
Anti-androgen
MOA: nonsteroidal androgen receptor antagonists->inhibit ligand binding of receptor and translocation of the androgen receptor-ligand complex to the nucleus
Rarely used alone; used in combo w/ GnRH agonist during first few weeks of treatment to prevent excess androgen production
Tx: prostate cancer (must be given w/ GnRH analog)
SE: gynecomastia, liver toxicity (less w/ bicalutamide) |
|
|
Term
Bromocriptine
Cabergoline
Pergolide
Quinagolide |
|
Definition
MOA: dopamine D2 receptor agonist-> activate Gqi D2 receptor
Use: tx of pituitary adenomas-> decrease prolactin secretion and cause decrease in GH release |
|
|
Term
|
Definition
Circulating estrogen
Rarely used pharmacologically-> high 1st pass effect |
|
|
Term
Ethinyl estradiol
Ethynodiol diacetate
Quinestrol
Mestranol |
|
Definition
Ethinylated estrogens
Ethinyl decreases 1st pass effects (poor hepatic enzyme substrate) and increases oral bioavailability
High potency
Use in oral contraceptions
Benefits: decreased pregnancies associated w/ pathology, osteoporosis, vasomotor symptoms, CV disease, vaginitis, and skin thinning
SE: thromboembolic events (esp in smokers, breast/endometrial carcinoma) |
|
|
Term
|
Definition
Conjugated estrogen
Less potent-> less of a breast cancer risk
Use in postmenopausal replacement therapy
Benefits: decreased pregnancies associated w/ pathology, osteoporosis, vasomotor symptoms, CV disease, vaginitis, and skin thinning
SE: thromboembolic events (esp in smokers, breast/endometrial carcinoma) |
|
|
Term
|
Definition
|
|
Term
|
Definition
Selective estrogen receptor modifiers
MOA: mixed estrogen agonist/antagonist
Anti-estrogen: breast cancer tissue
Pro-estrogen: endometrium, bone
Tx breast cancer. osteoporosis
SE: endometrial cancer |
|
|
Term
|
Definition
Selective estrogen receptor modifiers
MOA: mixed estrogen agonist/antagonist
Anti-estrogen: breast cancer tissue, endometrium
Pro-estrogen: bone
Tx breast/endometrial cancer, osteoporosis |
|
|
Term
|
Definition
Antiestrogen
MOA: estrogen antagonist effect in pituitary-> blocks negative feedback by estrogen, allowing increase in LH/FSH
Use: induce ovulation |
|
|
Term
|
Definition
Antiestrogen
MOA: full estrogen receptor antagonist in all tissues
Use: tx breast cancer after tamoxifen therapy |
|
|
Term
|
Definition
Estrogen synthesis inhibitors
MOA: suicide inhibitor of aromatase-> irreversible binding=> very potent
Tx: breast cancer
SE: osteoporosis |
|
|
Term
|
Definition
Estrogen synthesis inhibitors- non-steroidal
MOA: reversible aromatase inhibitor
Tx: breast cancer |
|
|
Term
|
Definition
Hydroxyprogesterone caproate- parenteral only
Medroxyprogesterone acetate (MPA)- can be used orally=> postmenopausal replacement therapy
Megestrol acetate- derived from MPA=> antineoplastic and increases appetite in tx of breast/endometrial cancer
Use in oral contraceptives-> increase cervical mucosal thickening and endometrial alterations to impair implantation |
|
|
Term
Norethindrone
Norgestrel
Norgestimate
Desogestrel
Norethynodrel
Gestodene |
|
Definition
Progestin analog
Potent; oral bioavailability
Use in oral contraceptives-> increase cervical mucosal thickening and endometrial alterations to impair implantation
Less effective than mixed contraceptives, but good for those w/ breast cancer risks and nursing mothers
Gestodene = androgenically neutral
SE: acne, weight gain, decrease HDL, increase LDL-> less w/ Norgestimate, Desogestrel, and Gestodene |
|
|
Term
|
Definition
Progestin agonist
Spironolactone derivative-> MR antagonist |
|
|
Term
| Combination Oral Contraceptives |
|
Definition
Estrogen + Progestin
Estrogen = pro-proliferation
Progestin = pro-differentiation
MOA: suppress LH/FSH and ovulation
Can have mono-, bi-, or triphasic=> progestin content varies w/ phase
Allows fewer androgen-like SE and blood lipid profile than w/ single progestin concentration |
|
|
Term
|
Definition
MOA: monoclonal Ab against HER2/erbB-2/NEU oncogene-> inhibist tyrosine kinase activity
Tx: breast cancer |
|
|
Term
|
Definition
MOA: monoclonal Ab against EGF receptor HER1/erbB-1
Tx: breast, colorectal, and head/neck cancer |
|
|
Term
Sildenafil
Tadalafil
Vardenafil |
|
Definition
MOA: cGMP 5-phosphodiesterase inhibitors-> prolonged cGMP elevation = increased NO induced vasodilation
SE: cardiac, ocular |
|
|
Term
|
Definition
PGE1 analog
Smooth muscle relaxant-> treatment of impotence
Intraurethral application, intracavernosal injection
Should not be used for intercourse during pregnancy-> can induce uterine contractions |
|
|
Term
|
Definition
Tx: anaerobic protozoal parasites-> T. vaginalis
Increasing resistance |
|
|
Term
Ciprofloxacin
Levofloxacin
Ofloxacin |
|
Definition
Fluoroquinolones
Tx: chlamydia, gonorrhea
C/I: pregnancy |
|
|
Term
|
Definition
| Tx: syphilis and sensitive gonococcal strains |
|
|
Term
|
Definition
3rd gen cephalosporin
Tx: gonorrhea |
|
|
Term
|
Definition
Tetracycline
Tx: chlamydia (C. trachomatis)
Fecal elimination-> safe for pts w/ renal impairment
C/I: pregnancy |
|
|
Term
|
Definition
Tx: chlamydial infections, nongonococcal urethritis
Can be given as a one time, single dose |
|
|
Term
Acyclovir
Valacyclovir
Famciclovir |
|
Definition
|
|
Term
|
Definition
|
|
