Term
|
Definition
Acts on target tissues (esp liver) through JAK2 (a TK) to initiated signalling pathways;
Production of IGF-1(&2) to exert effects;
Dec insulin sens, inc lipolysis, inc protein synth, inc epiphyseal growth;
Secretion stimulated by hypoglycemia, insulin;
Physiologic pulsatile release |
|
|
Term
|
Definition
hGH;
Replacement therapy in children;
Tx child - pituitary dwarfism (d/c when growth stops);
Tx adults - CV dz mortality, AIDS-associated wasting;
SE child (fewer) - leukemia, inc ICP, nausea;
SE adult - carpal tunnel, peripheral edema, arthralgia, myalgia;
CI - leukemia tx |
|
|
Term
|
Definition
hGH + methionine;
Replacement therapy in children;
Tx child - pituitary dwarfism (d/c when growth stops);
Tx adults - CV dz mortality, AIDS-associated wasting;
SE child (fewer) - leukemia, inc ICP, nausea;
SE adult - carpal tunnel, peripheral edema, arthralgia, myalgia;
CI - leukemia tx |
|
|
Term
| Sermorelin acetate (Geref) |
|
Definition
GHRH, short form;
First 29 AA;
Diagnostic uses |
|
|
Term
|
Definition
GH receptor antagonist;
Dec IGF-1;
+Polyethylene glycol (PEG) to dec renal cl, inc t1/2;
Tx acromegaly |
|
|
Term
|
Definition
IGF-1 + IGFBP-3 (both recombinant humaniod);
Binding protein - inc t1/2 of IGF-1;
Tx IGF-deficiency |
|
|
Term
|
Definition
Rises during pregnancy til birth;
Lvls maintained for breast feeding, drop if no feeding;
Know symptoms of hyperprolactemia |
|
|
Term
|
Definition
D2 receptor agonist;
Dec prolactin production @ ant. pituitary;
Cheap
Tx hyperprolactinemia from pit. adenoma, Parkinson's (primary use) |
|
|
Term
|
Definition
D2 receptor agonist;
Dec prolactin production @ ant. pituitary;
Inc affinity, inc t1/2;
Tx hyperprolactinemia from pit. adenoma |
|
|
Term
|
Definition
Somatostatin analog;
Dec secretion of GH and TSH;
Short t1/2;
Tx gigantism/acromegaly;
SE - diarrhea, nausea, abdominal pain |
|
|
Term
| Lanreotide (Somatuline LA) |
|
Definition
Somatostatin analog;
Dec secretion of GH and TSH;
Long-acting;
Tx gigantism/acromegaly;
SE - diarrhea, nausea, abdominal pain |
|
|
Term
|
Definition
Glycoprotein hormone released in ant. pituitary;
Stim by TRH and dec iodine, inhibited by somatostatin;
Inc release of T4,T3 secretion, THEN synthesis;
Thyroid hypertrohpy, hyperplasia;
High lvls - stim of phospholipase C - inc cystolic Ca;
Admin for dx tool to distinguish 1* from 2* hypothyroid |
|
|
Term
|
Definition
Glycoprotein hormone released in ant. pituitary;
Men @ Leydig cells to stimulate androgen production, spermatogenesis;
Women, a spike will induce ovulation;
Release stim by GnRH |
|
|
Term
| Follicle-stimulating hormone (FSH) |
|
Definition
Glycoprotein hormone released in ant. pituitary;
Release stim by GnRH;
Female - gametogenesis and follicle development, used in replacement;
Male - initiation and maintenance of spermatogenesis |
|
|
Term
|
Definition
FSH + LH;
Extracted from post-menopausal urine;
IM admin;
Tx female infertility |
|
|
Term
|
Definition
SC admin;
Tx female infertility |
|
|
Term
|
Definition
rFSH;
SC admin;
Tx female infertility |
|
|
Term
| Chorionic gonadotropin (CG) |
|
Definition
Secreted by placenta in early pregnancy;
Detected in urine to dx pregnancy;
Extracted from prego's urine - Tx female infertility |
|
|
Term
|
Definition
Corticotropin (ACTH)
alpha-MSH and beta-MSH (melanocyte stimulating hormone) |
|
|
Term
| Melanocyte-stimulating hormones (MSH) |
|
Definition
POMC-deriv from ant. pituitary;
Inc production concurrent w/ inc ACTH production leads to hyperpigmentation |
|
|
Term
| Growth hormone-releasing hormone (GHRH) |
|
Definition
Hypothalamic stimulatory hormone;
Inc GH release;
Negative feedback by rising GH lvls;
Used to determine the cause of GH deficiency |
|
|
Term
| Gonadotropin-Releasing Hormone (GnRH) |
|
Definition
Hypothalamic stimulatory hormone;
Stimulates FSH, LH production; |
|
|
Term
| Gonadorelin hydrochloride (Factrel) |
|
Definition
Synthetic GnRH;
SHORT t1/2;
Diagnostic testing to diff pituitary and hypothalamic lesions in pts w/ hypogonadotropism |
|
|
Term
|
Definition
GnRH analog;
Inc t1/2, inc receptor binding - induces receptor downregulation;
Tx prostate cancer, uterine fibroids |
|
|
Term
| Thyrotropin-releasing hormone (TRH) |
|
Definition
Diagnostic testing of thyroid function;
Stimulates TSH and prolactin |
|
|
Term
| Corticotropin-releasing hormone (CRH) |
|
Definition
| Diagnostic testing to diff Cushings Dz from ectopic ACTH syndrome |
|
|
Term
|
Definition
POMC-deriv(39AA) from ant. pituitary;
Works at G-protein coupled receptor to stimulate AC to produce cAMP;
Use - test integrity of HPA axis |
|
|
Term
| Regulation of ACTH release (4 routes) |
|
Definition
Circadian rhythm;
(+) stress (overriding)
(-) cortisol @ pit and hypothalamus;
(-) ACTH |
|
|
Term
| Natural ACTH (H.P. Acthar Gel) |
|
Definition
From animal sources, POMC peptide;
Use - test integrity of HPA axis |
|
|
Term
|
Definition
Synthetic ACTH (24 AA);
Preferred to natural product b/c no vasopressin activity;
Use - test integrity of HPA axis |
|
|
Term
|
Definition
Produced in adrenal cortex;
Stimulate gluconeogenesis, glycogenolysis;
Anti-inflammatory, acts by dec Phospholipase A2, dec cytokines, dec histamine;
Periphery - [oppose insulin] dec glu use, inc proteolysis, lipolysis;
Mostly delayed effects; |
|
|
Term
|
Definition
Suppression of ACTH and TSH production;
Inc lipolysis, redistribute fat;
Inc DM risk (opposes insulin);
Peptic ulcers;
CNS - arousal, euphoria, insomnia, inc motor activity;
Blood - inc Hgb RBCs PMNs, dec lymphocytes eosinophils monocytes basophils;
Men - hypogonadism;
Women - stops ovulation, dysmenorrhea, osteoporosis (post-men);
Children - inh IGF-1, dec GH, osteoporosis;
Lose Ca++ |
|
|
Term
|
Definition
Produced in adrenal cortex (10mg/day);
Stimulate gluconeogenesis, glycogenolysis;
Anti-inflammatory, acts by dec Phospholipase A2, dec cytokines, dec histamine;
Periphery - [oppose insulin] dec glu use, inc proteolysis, lipolysis;
Mostly delayed effects;
90% bound to CBP or albumin;
Converted (kidney, colon, salivary glands) to cortisone - won't bind MC receptors; |
|
|
Term
| Hydrocortisone (Hydrocortone) |
|
Definition
Glucocorticoid;
Short t1/2;
IM, IV, oral admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma, skin dz, IBD |
|
|
Term
| Cortisone acetate (Cortone acetate) |
|
Definition
Glucocorticoid;
Short t1/2;
IM, IV, oral admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma |
|
|
Term
|
Definition
Glucocorticoid;
Med t1/2;
Oral admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma, RHEUMATIC dz, RENAL dz, IBD, HEPATIC dz |
|
|
Term
| Prednisolone (Delta-Cortef) |
|
Definition
Glucocorticoid;
Med t1/2;
IM, IV admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma, HEPATIC dz |
|
|
Term
| Methylprednisolone (Medrol) |
|
Definition
Glucocorticoid;
Med t1/2;
IM, IV, oral admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma;
Gen immunosuppression |
|
|
Term
|
Definition
Glucocorticoid;
Long t1/2;
IM, IV, topical, oral admin;
Tx replacement therapy for adrenal insuff. and CAH, ALL, lymphoma, OCULAR DZ |
|
|
Term
| Betamethasone (Celestone) |
|
Definition
Glucocorticoid;
Long t1/2;
Oral, topical admin;
Tx asthma |
|
|
Term
| Triamcinolone (Aristocort) |
|
Definition
Glucocorticoid;
Long t1/2;
Oral, topical admin;
Tx asthma |
|
|
Term
|
Definition
Glucocorticoid;
Dec mucus secretion, dec bronch hyperactivity;
Tx asthma, COPD, IBD |
|
|
Term
|
Definition
Mineralocorticoid (0.125 mg/day);
Na/water retention, K&H secretion @DCT;
Inc ECF, hypoK (muscle weakness), alkalosis;
Inc synthesis of adrenergic receptors;
Stimulated by angII, inc K, ACTH;
SE - edema, HTN, cardiomyopathy, CHF, hemorrhage; |
|
|
Term
| Fludrocortisone (Florinef) |
|
Definition
Mineralocorticoid - synthetic Aldo;
Na/water retention, K&H secretion @DCT;
Inc ECF, hypoK (muscle weakness), alkalosis;
SE - edema, HTN, cardiomyopathy, CHF, hemorrhage; |
|
|
Term
|
Definition
| Aldoesterone antagonist - K-sparing diuretic; |
|
|
Term
| Aminoglutethimide (Cytadren) |
|
Definition
Adrenocortical "inhibitor";
Inhibits CYP450 - Dec cortisol production;
Tx Cushings |
|
|
Term
|
Definition
Antifungal - secondary Adrenocortical "inhibitor";
Inhibits CYP450 - Dec cortisol production;
Inh testosterone production;
Tx Cushings, systemic fungal infections |
|
|
Term
|
Definition
Estradiol, estrone, estriol;
70% bound to SHBG;
Reproductive - birth control, inc libido;
MC - closes epiphysis, dec osteoclasts, inc bone maturation, inc muscle content;
Hepatic - inc clotting factors, binding proteins;
Lipids - inc HDL, dec LDL;
High first pass met, dec p.o. efficacy;
Tx - osteoporosis, prostate cancer, HRT;
SE - endomet. cancer risk, thromboembolism, HTN, GI, CHD; |
|
|
Term
|
Definition
Locations - female reproductive tract;
affects transcription |
|
|
Term
|
Definition
Locations - prostate and ovary;
affects transcription |
|
|
Term
| Ethinyl estradiol (Estinyl) |
|
Definition
Estrogen - synthetic 17alpha;
Dec first pass met;
Tx CONTRACEPTION (most common Rx) |
|
|
Term
| Mestranol (ethinyl estradiol 3-methylether) |
|
Definition
Estrogen - synthetic 17alpha;
Dec first pass met;
Tx CONTRACEPTION (most common Rx) |
|
|
Term
| Conjugated esters of estrogen (Premarin) |
|
Definition
Pregnant mare urine;
IM injection - dec first pass met.;
Dissolved in oil - absorbed over several weeks;
Tx sypmtoms of menopause, HRT |
|
|
Term
| Esters of estradiol (Delestrogen) |
|
Definition
IM injection - dec first pass met.;
Dissolved in oil - absorbed over several weeks;
Tx sypmtoms of menopause, HRT |
|
|
Term
|
Definition
Crystalline estrone sulfate;
Estrogen formulation for standard tx's |
|
|
Term
|
Definition
Non-steroidal estrogen;
Dec first pass met.;
Tx prostate cancer, birth control;
Can be admin transdermally;
SE - teratogenic! |
|
|
Term
|
Definition
Non-steroidal estrogen;
Dec first pass met.;
Tx prostate cancer, birth control;
Can be admin transdermally; |
|
|
Term
|
Definition
Rises after ovulation to maintain pregnancy;
Bound to transcortin for transport;
Reproductive - dec uterine contraction & oviduct motility, thick cervical mucus, alveolobular dev (breast);
Lipids - dec HDL, inc LDL;
Metabolic - inc insulin, inc lipoprotein lipase;
SE - CAD, CNS depressant, acne, weight gain |
|
|
Term
|
Definition
Synthetic progesterone;
Tx endometrial cancer, component of birth control |
|
|
Term
|
Definition
Synthetic progesterone;
Tx endometrial cancer, component of birth control |
|
|
Term
|
Definition
Synthetic progesterone;
Morning-after pill, first 72 hours post-intercourse;
Tx endometrial cancer, component of birth control |
|
|
Term
|
Definition
SERM;
Agonist in bone, brain, liver;
Antagonist in breast, endometrium;
Tx breast & endometrial cancers |
|
|
Term
|
Definition
SERM;
Agonist in bone, brain, liver;
Antagonist in breast, endometrium;
Tx breast & endometrial cancers |
|
|
Term
|
Definition
SERM;
Agonist in bone, brain, liver;
Antagonist in breast, endometrium;
Tx breast & endometrial cancers |
|
|
Term
|
Definition
Anti-estrogen;
Antagonist in all tissues (ER-alpha & -beta);
Ovulation induction via reflex inc GnRH;
Tx infertility |
|
|
Term
|
Definition
Anti-estrogen;
Antagonist in all tissues (ER-alpha & -beta);
Ovulation induction via reflex inc GnRH;
Tx infertility |
|
|
Term
| Mifepristone (Mifeprex) - RU 486 |
|
Definition
Anti-progestin;
Blocks P receptor for the termination of gestation in first 7 weeks |
|
|
Term
|
Definition
Anti-progestin - pure antagonist;
Blocks P receptor for the termination of gestation |
|
|
Term
|
Definition
Aromatase inhibitor;
Block production of estrogens from androgens;
Tx breast cancer after Tamoxifen fails |
|
|
Term
|
Definition
Aromatase inhibitor;
Block production of estrogens from androgens;
Tx breast cancer after Tamoxifen fails |
|
|
Term
|
Definition
Androgen;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, PMS, anabolic steroids;
SE - masculinization, virilization, CAD, hepatic carcinoma, suppression of LH & FSH |
|
|
Term
| Testosterone trasdermal (Testoderm) |
|
Definition
Testosterone derivative;
Good efficacy due to no first pass met., "better" than oral or IM routes;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
| Methyltestosterone (Oretin methyl) |
|
Definition
Testosterone derivatve;
Oral, short acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
|
Definition
Testosterone derivatve;
IM, short acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
| Testosterone cypionate (Depo-testosterone) |
|
Definition
Testosterone derivatve;
IM, long acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
| Testosterone enanthate (Delatestryl) |
|
Definition
Testosterone derivatve;
IM, long acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
| Fluoxymesterone (Halotestin) |
|
Definition
Testosterone derivatve;
Oral, short acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
|
Definition
Testosterone derivatve;
IM, long acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx ENDOMETRIOSIS, elderly men (inc muscle mass), IM injection for HRT, endometriosis, PMS, anabolic steroids; |
|
|
Term
| Cyproterone acetate (Cyprostat) |
|
Definition
Androgen receptor antagonist;
Competes with DHT;
Tx acne, baldness, virilizing syndrome, sexual deviants (dec libido) |
|
|
Term
|
Definition
Androgen receptor antagonist;
Tx prostate cancer;
SE - hepatotox |
|
|
Term
|
Definition
Androgen receptor antagonist;
Tx prostate cancer;
SE - hepatotox |
|
|
Term
|
Definition
Androgen receptor antagonist;
Tx prostate cancer;
Less hepatotoxic |
|
|
Term
|
Definition
(also Propecia);
Blocks testo conversion (5alpha reductase) to DHT;
Tx BPH, male-pattern baldness;
SE - teratogenic |
|
|
Term
|
Definition
| Insulin-dependent glucose transporter |
|
|
Term
|
Definition
Animal insulin used for replacement therapy;
Differs from human insulin at 1 AA;
Dec use due to the equally affordable human insulin;
Antibodies to drug can develop |
|
|
Term
|
Definition
Animal insulin used for replacement therapy;
Differs from human insulin at 3 AA;
Dec use due to the equally affordable human insulin;
Antibodies to drug can develop |
|
|
Term
|
Definition
Animal insulin used for replacement therapy;
Differs from human insulin at 3 AA;
Dec use due to the equally affordable human insulin;
Antibodies to drug can develop |
|
|
Term
|
Definition
Insulin activity w/ intermed duration;
Injected 2x daily |
|
|
Term
|
Definition
Intermed-duration insulin combined w/ short-acting injected before meals;
Dec post-prandial spike and provides longer-acting insulin |
|
|
Term
|
Definition
30% semilente and 70% ultralente zinc insulin crystals;
Provides short and long term benefits; |
|
|
Term
|
Definition
| Short acting insulin crystals included in 'Lente' preparation; |
|
|
Term
|
Definition
Long acting insulin crystals included in 'Lente' preparation;
Long acting = large crystals |
|
|
Term
|
Definition
Recombinant "regular" human insulin;
Made in bacteria or yeast;
Limited anti-insulin Ab's |
|
|
Term
|
Definition
Recombinant "regular" human insulin;
Synthesized beg. with porcine insulin and replacing the 1 different AA;
Limited anti-insulin Ab's |
|
|
Term
|
Definition
Short acting insulin prep;
Synthesized beg. w/ Humulin, 1 AA replaced (via rDNA) to prevent hexamer formation w/ zinc;
End product - faster onset, short t1/2 |
|
|
Term
|
Definition
Short acting insulin prep;
Synthesized beg. w/ Humulin, 1 AA replaced (via rDNA) to prevent hexamer formation w/ zinc;
End product - faster onset, short t1/2 |
|
|
Term
| Insulin glargine (Lantus) |
|
Definition
Long acting insulin prep;
1 AA substituted, + Arg at C-term;
Prepared in acidic solution - Crystals precipitate upon injection - SLOW ABSORPTION;
PK - Slow release - long plateau w/ no peaks; |
|
|
Term
| Insulin detemir (Levemir) |
|
Definition
Long acting insulin prep;
1 AA substituted;
Prepared in acidic solution - Crystals precipitate upon injection - SLOW ABSORPTION;
PK - Slow release - long plateau w/ no peaks; |
|
|
Term
| Insulin glulisine (Apidra) |
|
Definition
Short acting insulin prep;
Synthesized beg. w/ Humulin, 2 AAs replaced (via rDNA) to prevent hexamer formation w/ zinc;
End product - faster onset, short t1/2 |
|
|
Term
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
| Chlorpropamide (Diabinese) |
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
2nd Gen Sulfonylurea - 10-100X more potent;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
2nd Gen Sulfonylurea - 10-100X more potent;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
2nd Gen Sulfonylurea - 10-100X more potent;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
2nd Gen Sulfonylurea - 10-100X more potent;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
Meglitinide - benzoic acid deriv;
Very rapid GI absorption;
Inc insulin secretion;
Short t1/2, used for post-prandial control
Tx DM, promote hypoglycemia;
SE - severe hypoglycemia; |
|
|
Term
|
Definition
Meglitinide - benzoic acid deriv;
Very rapid GI absorption;
Inc insulin secretion;
Short t1/2, used for post-prandial control
Tx DM, promote hypoglycemia;
SE - severe hypoglycemia |
|
|
Term
|
Definition
Biguanide;
GI absorption - little first pass met.;
Dec hepatic glucose production;
No hypoglycemia, NO INSULIN AXN;
SE - BLACK BOX lactic acidosis |
|
|
Term
|
Definition
Thiazolidindione;
GI absorption - little first pass met.;
Bind PPAR-gamma receptor, inc insulin sensitivity;
Tx DM, promote hypoglycemia;
SE - BLACK BOX MI risk |
|
|
Term
|
Definition
Thiazolidindione;
GI absorption - little first pass met.;
Bind PPAR-gamma receptor, inc insulin sensitivity;
Tx DM, promote hypoglycemia; |
|
|
Term
|
Definition
Alpha-glucosidase (brush border enzyme) inhibitor;
Dec carbohydrate (starch) absorption;
Dec post-prandial glu spike;
Tx DM, promote hypoglycemia; |
|
|
Term
|
Definition
Alpha-glucosidase (brush border enzyme) inhibitor;
Dec carbohydrate (starch) absorption;
Dec post-prandial glu spike;
Tx DM, promote hypoglycemia; |
|
|
Term
|
Definition
Incretin- Works thru GIP/GLP-1 mechanisms, more potent;
Synthetic version of exendin-4 (Gila monster);
Inc insulin, dec glycogenolysis, dec gastric emptying, dec appetite, dec glucagon, some inc in beta cells - hypoglycemia!; |
|
|
Term
|
Definition
'Incretin';
Inhibits dipeptidyl peptidase-4, inh inactivation of Incretins (GIP/GLP-1);
-> Inc insulin, dec glycogenolysis, dec gastric emptying, dec appetite, dec glucagon, some inc in beta cells - hypoglycemia!; |
|
|
Term
|
Definition
Amylin analog;
Dec gastric emptying, inc satiety (@hypothalamus), inh glucagon;
Weight loss and less insulin req.;
Tx DM1 and DMII |
|
|
Term
Diazoxide (Proglycem)
(ASMT 10 = CAPS ONLY) |
|
Definition
direct vasodilator, HYPERGLY AXN;
tx HTN crisis, HYPOGLYCEMIA, INOPERABLE INSULINOMAS;
INH INSULIN SECRETION;
SE tachycardia, fluid retention, palpitations, HYPERGLYCEMIA |
|
|
Term
|
Definition
Somastatin analog - long acting;
Inh insulin, glucagon, GH, and TSH release;
Tx insulinomas, glucagonomas, acromegaly |
|
|
Term
Parathyroid hormone
(+ 3 functions) |
|
Definition
Activates AC to inc cAMP;
Inc plasma Ca by [1] inc bone resorption, [2] inc kidney reabsorption, [3] inc active VitD/calcitriol; |
|
|
Term
|
Definition
hPTH[1-34];
Activates AC to inc cAMP;
Inc plasma Ca by [1] inc bone resorption, [2] inc kidney reabsorption, [3] inc active VitD/calcitriol;
Tx hypoparathyroidism |
|
|
Term
|
Definition
Activates AC to inc cAMP;
Inc plasma Ca by [1] inc bone resorption, [2] inc kidney reabsorption, [3] inc active VitD/calcitriol;
Tx hypoparathyroidism |
|
|
Term
Synthetic human calcitonin (hCT)
(+ 3 functions) |
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Definition
Dec plasma Ca by [1] dec bone resorption, [2] dec kidney reabsorption, [3] dec active VitD/calcitriol;
Dec osteoclast surface area;
"Calcitonin tones down plasma Ca lvls";
Tx hypercalcemia, Paget's dz, osteoporosis |
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Term
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Definition
Natural calcitonin from salmon;
Dec plasma Ca by [1] dec bone resorption, [2] dec kidney reabsorption, [3] dec active VitD/calcitriol;
Dec osteoclast surface area;
"Calcitonin tones down plasma Ca lvls";
Tx hypercalcemia, Paget's dz, osteoporosis |
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Definition
Natural calcitonin from salmon;
Dec plasma Ca by [1] dec bone resorption, [2] dec kidney reabsorption, [3] dec active VitD/calcitriol;
Dec osteoclast surface area;
"Calcitonin tones down plasma Ca lvls";
Tx hypercalcemia, Paget's dz, osteoporosis |
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Definition
Inc plasma Ca by...
Inc abs./uptake of P and Ca(primary);
Inc calbindin;
Inc kidney reabsorption;
Inc bone resorption |
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Definition
Calcitriol mimetic;
Vit D3 from fish liver oils;
Remains in lipid stores for months;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol mimetic;
sim to cholesterol;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol mimetic;
after irradiation - Vit D2;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol mimetic;
Conv in body to calcitriol;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol analog;
Tx PSORIASIS(better than GCs), rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol analog - Reduced Vit D2;
Injection, nasal spray;
Less active, use inc dose;
Tx OSTEOPOROSIS, rickets, osteomalacia, hypoparathyroid |
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Definition
Calcitriol analog;
MOA - dec PTH secretion;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Calcitriol analog;
MOA - dec PTH synthesis via gene expression;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Definition
Inc plasma Ca by...
Inc abs./uptake of P and Ca(primary);
Inc calbindin;
Inc kidney reabsorption;
Inc bone resorption;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
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Term
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Definition
1st Gen. Bisphosphonate;
Less effective orally;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, hypercalcemia;
SE - via IV admin, osteonecrosis of jaw (less common in 1st gen) |
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Definition
2nd Gen. Bisphosphonate - more potent;
Most common Rx for post-meno Tx;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis;
SE - via IV admin, osteonecrosis of jaw (less common in 2nd gen), irritation of esophagus |
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Definition
2nd Gen. Bisphosphonate - more potent;
Less effective orally;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, hypercalcemia;
SE - via IV admin, osteonecrosis of jaw (less common in 2nd gen), irritation of esophagus |
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Definition
2nd Gen. Bisphosphonate - more potent;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis;
SE - via IV admin, osteonecrosis of jaw (less common in 2nd gen), irritation of esophagus |
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Definition
3rd Gen. Bisphosphonate - HIGH POTENCY;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, BONE CANCER;
SE - via IV admin, osteonecrosis of jaw! |
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Definition
3rd Gen. Bisphosphonate - HIGH POTENCY;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, BONE CANCER;
SE - via IV admin, osteonecrosis of jaw! |
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Definition
Calcimimetic - Ca sensing receptor mimetic;
Binds allosterically to the receptor, suppresses PTH;
Tx hyperparathyroid w/ PT-carcinoma |
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Definition
Binds Ca;
Cavity prophylaxis - benefits only if present during tooth development;
Prevent blood clotting;
Prevent osteoporosis;
SE osteosclerosis, mottled enamel;
NO cancer risk |
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Term
| Desiccated animal thyroid preps |
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Definition
T4 and T3;
Not preferred b/c of high variability;
Causes growth, inc metabolism, inc HR;
Must monitor lvls closely;
Calorigenic, inc HR, cardiac contraction force |
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Term
| Liothyronine sodium (Cytomel tablets, Triostat injectable) |
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Definition
L-T3
Note oral or injectable;
Calorigenic, inc HR, cardiac contraction force |
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Term
| Carbimazole (Neo-mercazole) |
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Definition
Thioureylene - anti-thyroid drug;
Inh I organification(via peroxidases), can't bind to thyroglobulin;
Tx hyperthyroidism |
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Definition
Inh periph (liver, kidney, pituitary, brain) conv of T4->T3 via 5'-deiodinase block;
Tx hyperthyroidism (off-label) |
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Definition
Inh periph (liver, kidney, pituitary, brain) conv of T4->T3;
Tx hyperthyroidism (off-label) |
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Definition
Anti-Protozoal;
Activation via enzymatic reduction;
Blocks pyruvate:ferrodoxone oxidoreductase;
90% bioavail, BBB penetration, low protein binding;
Tx - trichomonas, entamoeba h., giardia, anaerobes (B. fragilis, C. diff);
SE - GI, HA, metallic taste, dizziness, disulfriam-like, anorexia, neuro tox |
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Definition
Anti-Protozoal;
Inhibits electron transport, dec pyrimidine synth;
99% protein bound, lipophillic, hydrophobic;
Tx pneumocystic pneumonia, toxoplasma, entamoeba, trichomonas, P. falciparum |
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Definition
Anti-Protozoal;
Poor abs - IV, inhaled admin;
Tx [2nd line]- pneumocystis, leishmania, trypanosoma;
SE [50%] - hypoT, hypoGly, blood dyscrasias, cardiotox, nephrotox |
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Definition
Anti-Protozoal;
Oral (50% bioavail) or IV admin;
Inh ornithine decarboxylase to block polyamine synth;
Tx - W. trypanosoma
SE - anemia, leucopenia, diarrhea, convulsions, GI, alopecia |
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Definition
Anti-Protozoal;
Poor abs;
Aminoglycoside Ab;
Tx - entamoeba, tapeworms, leishmanias, giardia (pregnancy);
SE - diarrhea, iodine tox;
CI - renal dz |
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Definition
Anti-Protozoal;
IV, IM admin;
MOA trypanothine redox system - rapid efflux of try. and GSH from cells, blocks try. reductase;
Tx - leishmaniasis;
SE - pancreatitis, myelosuppression, muscle pain |
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Term
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Definition
Anti-Protozoal;
Poor abs;
Tx - tapeworms, luminal trophozoites;
SE - diarrhea, iodine tox, GI (take w/ meals);
CI - optic neuropathy, renal dz, thyroid dz;
Preferred alternative is Paramomycin; |
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Definition
Anti-Protozoal;
Rapid exretion, IV admin;
Arsenic-containing, inh trypanothione reductase;
Tx trypanosoma brucei (E. african meningoencephalic stage);
SE [prevent w/ prednisone] - fever, reactive encephalopathy, peripheral neuropathy |
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Term
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Definition
Blood schizontocide;
Wide distribution, slow clearance (months);
Resistance - efflux at P-gp;
Tx - Plasmodium, non-GI amebiasis;
Prophylactic use;
SE - blurred vision (melanin binding, corneal deposits), retina pigmentation, hemolysis (if G6PD deficient); |
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Definition
Blood schizontocide;
Block DNA synthesis;
Tx - P. falci, gametes of P. vivax and P. malariae;
Poor therapeutic index;
SE - dec heart contract., dilate vessels, contract uterus, vertigo, hemolysis (if G6PD deficient),
Cinchonism - tinnitus, blurred vision, HA, dec hearing |
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Definition
Blood schizontocide and antiarrhythmic;
Block DNA synthesis;
Tx - severe P. falci, gametes of P. vivax and P. malariae;
SE - anticholinergic;
CI - AV heart block |
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Term
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Definition
Blood schizontocide;
Oral admin, 98% bound, excreted in bile;
Acts only @ asexual erythrocytic stages;
Block DNA synthesis;
Tx - P. falci, gametes of P. vivax and P. malariae;
SE - GI, vertigo, convulsions;
CI - BBs, chloroquine, quinine, quinidine, hx seizures |
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Term
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Definition
Blood schizontocide;
Acts only @ asexual erythrocytic stages;
HIGH absorption when admin w/ [fatty] food (CI!);
Tx - multi-resistant P. falci;
SE - prolonged QT interval, arrhythmias;
Variable absorption, time to peak [plasma], and elim |
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Term
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Definition
Blood schizontocide;
Variable oral abs;
Tx P. falci;
Dec cardiotox |
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Definition
Blood schizontocide - from Chinese herb;
Free radicals dmg macromolecules in Plasmodium;
Tx - severe chloro-resistant Plasmodium [falci], leishmania, toxoplasma, schistosomiasis |
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Definition
Blood schizontocide - Attack plasmodia in red blood cells preventing or terminating the clinical attack;
Acts only @ asexual erythrocytic stages; |
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Term
| Malarone (Atovaquone/proquanil) |
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Definition
Blood schizontocide - Attack plasmodia in red blood cells preventing or terminating the clinical attack;
Acts @ asexual erythrocytic stages and primary liver stages; |
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Definition
Tissue schizontocide, Gametocidal, Hypnozoitocidal;
Rapidly abs and conv to Carboxyprim.;
Tx - prophylaxis, P. vivax and P. ovale @ hepatic and gamete stages;
KILLS P. FALCI GAMETES;
CI - G6PD deficient (X-linked) leads to hemolytic anemia |
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Term
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Definition
Tissue schizontocide;
High abs;
Inhibits DHFR;
SE - dec hematopoeisis, megaloblastic anemia;
Never used alone, oft w/ Sulfadoxine |
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Term
| Fansidar (Sulfadoxine/Pyrimethamine) |
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Definition
Tissue schizontocide axn;
Tx - chloro-resistant P. falci, Toxoplasma;
SE - fatal cutaneous rxns (incl erythema multi, SJS, epidermal necrolysis); |
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Definition
Benzimidazole - Anti-helmintic;
Rapid met to albendazole sulfoxide;
Inh carb transport and microtubule assembly - immobilization and death;
Blocks larval development;
Tx helmintics - ascariasis, enterobius, hookworm;
SE - teratogen |
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Term
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Definition
Benzimidazole - Anti-helmintic;
Poor abs, highly bound;
Inh carb transport and microtubule assembly - immobilization and death;
Blocks larval development;
Tx helmintics - ascariasis, enterobius (pin), Trichuris (whip), hookworm;
SE - teratogen |
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Term
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Definition
Anti-helmintic;
Inc Ca++ perm - spastic paralysis;
Readily abs, hi first pass met, inc metabolites;
Tx - tapeworms, schistosomiasis, 3 forms of fluke;
SE - GI, HA;
CI - Carbamazepine & Phenobarbital dec bioavail; Cimetidine inc bioavail, ocular schistosomiasis; |
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Term
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Definition
Anti-helmintic;
Oral admin, no met, long t1/2 (slow cl);
Inc Cl perm. - inh glutamate and GABA-ergic channels - paralysis;
Tx - strongyloidiasis, onchocerca (rvr blindness);
SE - GI, itch, dizzy, inflamm rxn to dying bugs |
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Definition
Anti-helmintic;
Rapid GI abs;
Tx lymphatic filariasis;
SE - anorexia, nausea, HA |
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Term
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Definition
Anti-helmintic;
Poor abs;
Bind N receptors - depol blockade - spastic paralysis (bug falls off GI wall);
Tx - MONILIFORMIS, GI nematodes;
Dec SE due to localization of drug in GI - HA, dizziness, rash |
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Term
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Definition
Bile acid sequesterants;
Large tablet or powder, take w/ OJ;
Anionic, binds (-) bile acids in GI - inh bile recycling - liver excretes more chol;
Safe for children, hepatic dz;
Dec LDL by 25%;
SE - sandy texture, flatulence, hypertriglyceridemia, constipation, drug interaction; |
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Term
| Cholestyramine (Questran) |
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Definition
Bile acid sequesterants;
Powder form;
Anionic, binds (-) bile acids in GI - inh bile recycling - liver excretes more chol;
Safe for children, hepatic dz;
Dec LDL by 25%;
SE - sandy texture, flatulence, hypertriglyceridemia, constipation, drug interaction; |
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Definition
Bile acid sequesterants;
Tablet, more potent, forms hydrophilic gel, take w/ hi lvl of water;
Anionic, binds (-) bile acids in GI - inh bile recycling - liver excretes more chol;
Safe for children, hepatic dz;
Dec LDL by 25%;
SE - sandy texture, flatulence, hypertriglyceridemia, constipation, drug interaction; |
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Term
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Definition
Statin - inh HMG-CoA Reductase;
Prodrug, conv at CYP3A4, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases;
CI - renal dz |
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Term
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Definition
Statin - inh HMG-CoA Reductase;
Prodrug, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases, INTERAXN @ CYP3A4;
CI - renal dz |
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Term
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Definition
Statin - inh HMG-CoA Reductase;
Inc safety, low potency, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases;
CI - renal dz |
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Term
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Definition
Statin - inh HMG-CoA Reductase;
Inc safety, low potency, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases;
CI - renal dz |
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Term
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Definition
Statin - inh HMG-CoA Reductase;
Inc potency, dec renal cl, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases, INTERAXN @ CYP3A4; |
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Definition
Statin - inh HMG-CoA Reductase;
Most potent statin, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases;
CI - renal dz |
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Term
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Definition
Cholesterol absorption inhibitor;
Blocks internalization of NPC1L1 - dec chol abs by 50% - dec hepatic chol - upreg of LDL receptors - dec LDL by 18%;
SE - GI, fatuge, gallstones, Category C, inc liver enzymes;
Inc lvls in elderly, female;
CI - <10y.o., hepatic or renal insuff, lactation |
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Definition
Fibrate - anti-lipid;
Safe for renal, liver dz;
Activate PPAR-alpha - FA oxidation, inc biliary chol excretion (Dec TG by 50%);
Inc HDL (Apo-A1), no effect on LDL!;
Dec MI/CHD morbidity;
SE - gallstones, reflux, diarrhea, myopathy (if w/ statin);
Blocks hepatic met of all statins - inc metabolites; |
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Term
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Definition
Fibrate - anti-lipid;
Active met - fenofibric acid - glucaronidation;
Activate PPAR-alpha - FA oxidation, inc biliary chol excretion (Dec TG by 50%);
Inc HDL (Apo-A1), no effect on LDL!;
SE - gallstones, inc transaminases, dec GFR, azotemia;
CI - renal dz |
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Term
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Definition
Anti-lipid;
Dec FFA mobilization - dec TG & ApoB synth (dec VLDL), inc HDL transport, enhanced LPL;
Dec LDL by 25%, Dec TG by 50%, Dec Lp(a);
Dec CHD/MI incidence;
SE - hepatotox (inc enzymes), flushing, conjunctivitis, retinal detach, inc insulin resistance (a. nigricans), gout, dry skin, Category C, pruritis |
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Term
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Definition
Omega-3 FAs - ALA, EPA, DHA;
Dec TGs (35%), antiplatelet, hypotensive, antiarrhythmic;
Dec CHD |
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