Term
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Definition
Renin Inhibitor
For Hypertension |
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Term
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Definition
ACE inhibitors
For: Hypertension, heart failure, diabetic nephopathy, myocardial infraction |
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Term
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Definition
Angiotenin II recepter antagonist
For: Hypertension, heart failure, diabetic nephopathy, myocardial infraction, prevention of stroke |
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Term
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Definition
B-type natriuretic peptide
For: acutely decompensated heart failure |
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Term
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Definition
Vasopressin receptor 2 antagonist
For: Euvolemic hyponatremia, SIADH, Heart failure, cirrhotic asscites, autosomal domanant polycystic kidney disease |
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Term
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Definition
Carbonic Anhydrase inhibitor
Proximal convoluted tubule
For: High-altitude sickness, heart failure, epilepsy, glaucoma |
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Term
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Definition
Osmotic Diuretic
For: Cerebral edema, increased interoccular pressure, prophylaxis of oliguria in acute renal failure |
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Term
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Definition
Loop diuretic
Thick ascending limb
For: Hypertension, acute pulmonary edema, edema from heart failure (hepatic cirrhosis or renal disfunction),hypercalcemia, hyperkalemia |
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Term
| Hydrochlorothiazide (***thiazide) |
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Definition
Thiazide diuretics
Distal convoluted tubule
For: Hypertension, adjunct in edema states associated with heart failure, hepatic cirrhosis, renal dysfunction, corticosteroid or estrogen therapy |
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Term
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Definition
K+ Sparing diuretics
Collecting Duct
For: Hypertension, edema from heart failure (hepatic cirrhosis or renal disfunction), hypokalemia, primary aldosternonism, acne vulgaris, female hirsutism |
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Term
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Definition
K+ Sparing diuretics
Collecting Duct
For: Hypertension, Lidde's syndrome |
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Term
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Definition
K+ Sparing diuretics
Collecting Duct
For: Hypertension, Lidde's syndrome |
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Term
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Definition
Block HMG-coA reductase, the rate limiting enzyme in cholesterol synthesis in liver.
Reduce hepatic cholesterol synthesis, lowering intracellular cholesterol, which stimulates upregulation of LDL receptor and increases the uptake of non-HDL particles from the systemic circulation. |
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Term
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Definition
Fibric Acid derivatives
These agents activate a transcription factor called PPAR-alpha. This leads to elevations of lipoprotein lipase, which cleaves triglycerides from chylomicrons and VLDL particles.
There is a reduced rate of transfer of cholesterol from HDL to VLDL and chylomicrons, leading to increased HDL-cholesterol.
Need to monitor combined use with statins due to myotoxicity. Increases gall stones |
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Term
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Definition
Fibric Acid derivatives
These agents activate a transcription factor called PPAR-alpha. This leads to elevations of lipoprotein lipase, which cleaves triglycerides from chylomicrons and VLDL particles.
There is a reduced rate of transfer of cholesterol from HDL to VLDL and chylomicrons, leading to increased HDL-cholesterol.
Need to monitor combined use with statins due to myotoxicity. Increases gall stones |
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Term
| Cholestyramine, colestipol, colesevelam |
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Definition
Bile acid sequestrants
Large insoluble ion-exchange resins
Exchanges Cl- for negatively charged bile acids and escorts them out through the stool.
Must take with meals. Up to 20g per day.
Interferes with absorption of other drugs. Other drugs given >1 hour before or >4 hours after the resin
GI problems, bloating, constipation, absorbs vitamins (use supplements) |
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Term
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Definition
Decreases hepatic production of VLDL and of apo B
Nicotinic acid, vitamin B3. Use pharmacologic doses (more than nutritional)
Most develop flushing; dissipates with use. Can treat with aspirin
Many develop nausea requiring antacids or other agents.
Increases insulin resistance and uric acid formation which can exacerbate diabetes and gout. Jaundice, liver dysfunction also increased
AIM-High (niacin+statin) examined benefit of elevating HDL when LDL low. Halted early due to lack of efficacy |
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Term
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Definition
| Cholesterol Absorption Inhibitors |
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Term
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Definition
biguanide
Best used for insulin resistant obese type 2 diabetics.
Increases activity of AMP kinase in liver
Results in decreased production of glucose, fatty acids and cholesterol.
Increases glucose uptake in muscle
Reduces glucose levels without affecting insulin secretion
No risk of hypoglycemia due to excess insulin action
Often results in both weight loss and decreases in serum lipids
Adverse events include mild GI tract distress (minimized by gradually increasing dose) and lactic acidosis in those with hepatic, renal or respiratory insufficiency. (Lactic Acidosis) |
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Term
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Definition
Insulin Secretagogues
Act by inhibiting the K-ATP channel. This depolarizes the beta cell and leads to increased insulin release.
Used since the 1950s
Can results in hypoglycemia if excess insulin released
Causes weight gain. Best for nonobese patients.
Can cause “sulfa” rash |
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Term
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Definition
Insulin Secretagogues
Act by inhibiting the K-ATP channel. This depolarizes the beta cell and leads to increased insulin release.
Used since the 1950s
Can results in hypoglycemia if excess insulin released
Causes weight gain. Best for nonobese patients.
Can cause “sulfa” rash |
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Term
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Definition
Glucagon Like Peptide (GLP-1)
GLP-1 released from the GI tract with meals
Augments insulin release; inhibits glucagon release
Can inject direct agonist (exenatide) or block degradation by protease DPP-4 inhibitors (sitagliptin; saxagliptin; oral administration)
Minimal risk of hypoglycemia |
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Term
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Definition
Thiazolidinediones- PPARgamma activators
PPAR-gamma is a transcription factor
Makes cells more sensitive to insulin
Redirects fatty acids from liver/muscle to adipose tissue; decreases plasma triglycerides
Reduces inflammation
Adverse events are weight gain, edema, increased cardiovascular risk |
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Term
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Definition
Thiazolidinediones- PPARgamma activators
PPAR-gamma is a transcription factor
Makes cells more sensitive to insulin
Redirects fatty acids from liver/muscle to adipose tissue; decreases plasma triglycerides
Reduces inflammation
Adverse events are weight gain, edema, increased cardiovascular risk |
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Term
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Definition
Amylin Analogues
Amylin is released from beta cells with insulin
Slow gastric emptying (delays glucose peak) and decreases glucose release from liver (suppresses glucagon release)
Deficient in both type I and II diabetes
Decreases appetite through CNS effects
Injected subcutaneously pre-prandially
Significant GI tract adverse events. |
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Term
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Definition
Inhibition of Glucose Absorption; blockade of α-glucosidase
Decreases rate of starch breakdown in GI tract
Delays glucose absorption
Take with meal
Often combined with other drugs
Diminishes peak glucose and peak insulin
May lower triglycerides
No effects on weight
Can cause bloating, flatulance. More sugar for intestinal flora to digest.
Contraindicated for inflammatory bowel disease |
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Term
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Definition
(GH)*
Mechanism and Target : stimulate release of or replace growth hormone or insulin-like growth factor
Clinical Applications: Growth failure in children with GH deficiency, Turner’s syndrome, Prader-Willi Syndrome, Chronic kidney disease, idiopathic short stature, replacement of endogenous GH in adults with GH deficiency
Adverse Effects: increased intracranial pressure, pancreatitis, hyperglycemia, rapid growth of nevi (skin growth), peripheral edema, injection site reaction, headache, arthralgia (joint pain)
Contraindications: patients with closed epiphyses, active intracranial lesion, active malignancy, proliferative diabetic retinopathy |
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Term
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Definition
(GHRH)*
Mechanism and Target : same as above
Clinical Applications: diagnostic evaluation of plasma growth hormone
Adverse Effects: transient flushing, chest tightness, injection site reaction, antibody development
Contraindications: do not use with other drugs that affect pituitary hormones |
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Term
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Definition
Mechanism and Target : Same as above
Clinical Applications: Laron Dwarfism, GH deficiency with neutralizing antibodies
Adverse Effects: hypoglycemia, increased intracranial pressure, seizure, tonsillar hypertrophy, injection site reaction
Contraindications: patients with closed epiphyses, active malignancy, |
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Term
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Definition
Mechanism and Target : inhibit GH release
Clinical Applications: Acromegaly, flushing and diarrhea from carcinoid tumors, carcinoid crisis, diarrhea from vasoactive intestinal peptide secreting tumors, TSH-producing tumors
Adverse Effects: arrhythmias, bradycardia, hypoglycemia, gallstone formation, abdominal pain, constipation, diarrhea, nausea, vomiting
Contraindications: hypersentivity to octreotide |
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Term
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Definition
Mechanism and Target : antagonize GH receptor
Clinical Applications: Acromegaly
Adverse Effects: hypertension, peripheral edema, paresthesias, dizziness
Contraindications: hypersentivity to pegvisomant, known malignacy |
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Term
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Definition
Mechanism and Target : inhibit pituitary prolactin release
Clinical Applications: amenorrhea and galactorrhea from hyperprolactinemia, acromegaly, Parkinson's disease, premenstrual syndrome
Adverse Effects: dizziness, hypotension, abdominal cramps, nausea
Contraindications: hypersensitivity to ergot derivatives, uncontrolled hypertension, toxemia of pregnancy |
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Term
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Definition
Mechanism and Target : mixed V1/ V2 receptor antagonist
Clinical Applications: euvolemic and hypervolemic hyponatremia (low sodium), heart failure
Adverse Effects: hypertension, orthostatic hypotension, injection site reaction, hypokalemia, increased thirst, polyuria
Contraindications: concurrent use of P450 3A4 inhibitors |
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Term
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Definition
(TRH)*
Mechanism and Target :
Clinical Applications: diagnosis of thyroid function
Adverse Effects: seizure, anxiety, hyper- hypotension
Contraindications: None indicated |
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Term
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Definition
(TSH)*
Mechanism and Target :
Clinical Applications: adjunctive treatment of malignant tumor of thyroid gland
Adverse Effects: dizziness, headache, vomiting, nausea
Contraindications: adrenal insufficiency, coronary thrombosis |
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Term
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Definition
(ACTH 1-24)*
Mechanism and Target : stimulates adrenal cortisol and androgen production
Clinical Applications: diagnosis of adrenocortical function
Adverse Effects: increased intracranial hypertension, psuedotumor cerebri, seizures, heart failure, necrotizing vasculitis, shock, pancreatitis, peptic ulcer, hypokalemic alkalosis, induction of latent diabetes mellitus, bronchospasm
Contraindications: peptic ulcers, scleroderma, osteoporosis, systemic fungal infection, ocular herpes simplex, heart failure, hypertension, recent surgery, adrenocortical hyper-function or primary insufficiency, or Cushing’s syndrome |
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Term
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Definition
T4
Mechanism and Target : replace missing endogenous thyroid hormone with exogenous thyroid hormone
Clinical Applications: hypothyroidism, myxedema coma
Adverse Effects: hyperthyroidism, osteopenia, psuedotumor cerebri (benign intracranial hypertension), seizure, myocardial infarction
Contraindications: acute myocardial infarction, uncorrected adrenocortical insufficiency, untreated thyrotoxicosis |
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Term
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Definition
T3
Mechanism and Target : replace missing endogenous thyroid hormone with exogenous thyroid hormone
Clinical Applications: hypothyroidism, myxedema coma
Adverse Effects: hyperthyroidism, osteopenia, psuedotumor cerebri (benign intracranial hypertension), seizure, myocardial infarction
Contraindications: acute myocardial infarction, uncorrected adrenocortical insufficiency, untreated thyrotoxicosis |
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Term
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Definition
Iodide Uptake Inhibitors
Mechanism and Target : compete for iodide for uptake into thyroid gland follicular cells via sodium-iodide symporter, thereby decreasing intra-thyroid supply of iodide available for thyroid hormone synthesis
Clinical Applications: hyperthyroidism, radio-contrast agents
Adverse Effects: aplastic anemia, GI irritation
Contraindications: no major contraindications |
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Term
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Definition
Iodide Uptake Inhibitors
Mechanism and Target : compete for iodide for uptake into thyroid gland follicular cells via sodium-iodide symporter, thereby decreasing intra-thyroid supply of iodide available for thyroid hormone synthesis
Clinical Applications: hyperthyroidism, radio-contrast agents
Adverse Effects: aplastic anemia, GI irritation
Contraindications: no major contraindications |
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Term
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Definition
Iodide Uptake Inhibitors
Mechanism and Target : compete for iodide for uptake into thyroid gland follicular cells via sodium-iodide symporter, thereby decreasing intra-thyroid supply of iodide available for thyroid hormone synthesis
Clinical Applications: hyperthyroidism, radio-contrast agents
Adverse Effects: aplastic anemia, GI irritation
Contraindications: no major contraindications |
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Term
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Definition
radioactive Iodide
Mechanism and Target : radioactive iodide emits β-particles that are toxic to thyroid cells; High Iodide concentrations inhibits iodide uptake and organification via Wolff-Chaikoff effect
Clinical Applications: hyperthyroidism
Adverse Effects: may worsen opthalmyopathy in Graves’ Disease, hypothyroidism
Contraindications: pregnancy |
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Term
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Definition
High Concentrations
Mechanism and Target : radioactive iodide emits β-particles that are toxic to thyroid cells; High Iodide concentrations inhibits iodide uptake and organification via Wolff-Chaikoff effect
Clinical Applications: hyperthyroidism
Adverse Effects: may worsen opthalmyopathy in Graves’ Disease, hypothyroidism
Contraindications: pregnancy |
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Term
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Definition
PTU
Thioureylenes
Mechanism and Target : inhibits thyroid peroxidase and conversion of T4 to T3. methimazole inhibits thyroid peroxidase
Clinical Applications: hyperthyroidism
Adverse Effects: agranulocytosis, hepatotoxicity, vasculitis, hypothrombinemia, rash, arthralgias
Contraindications: pregnancy, breast feeding (methimazole) |
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Term
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Definition
Thioureylenes
Mechanism and Target : inhibits thyroid peroxidase and conversion of T4 to T3. methimazole inhibits thyroid peroxidase
Clinical Applications: hyperthyroidism
Adverse Effects: agranulocytosis, hepatotoxicity, vasculitis, hypothrombinemia, rash, arthralgias
Contraindications: pregnancy, breast feeding (methimazole) |
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Term
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Definition
5α- Reductase Inhibitors
Inhibit enzyme that converts testosterone to dihydrotestosterone
Used primarily for benign Prostatic hypertrophy
dutasteride (Avodart®)
finasteride (Proscar®; Propecia® for male pattern baldness) |
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Term
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Definition
STEROIDAL Aromatase inhibitors
Substrate analog
Irreversibly inactivates aromatase enzyme as “suicide inhibitor”
Can reduce estrogen levels
Used for breast cancer
Either as first line treatment
or as second line after tamoxifen
Do not increase risk of uterine cancer or deep vein thrombosis
Can cause hot flashes |
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Term
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Definition
NONSTEROIDAL Aromatase inhibitors
Interacts reversibly with heme groups of P450s, including aromatase
Can reduce estrogen levels
Used for breast cancer
Either as first line treatment
or as second line after tamoxifen
Do not increase risk of uterine cancer or deep vein thrombosis
Can cause hot flashes |
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Term
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Definition
Anti-Testosterone
androgen receptor antagonist
Used in prostate cancer |
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Term
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Definition
(SERM)
Agonist in bone
Used for osteoporosis
Agonist in liver
Benefits cholesterol balance
different from estrogens (decreased total cholesterol, decreased LDL, no increase HDL)
Agonist for vasomotor symptoms, deep vein thrombosis and stroke
No effects on endometrium
May be antagonist in breast
Current clinical trials for prevention of breast cancer |
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Term
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Definition
(SERM)
Used for infertility
Typically given for 5 days in follicular phase
Antagonist at the estrogen receptor in the anterior pituitary gonadotrope
Prevents negative feedback of LH and FSH
FSH, LH levels increase; better follicular recruitment; better ovulation
Major side effect is that it works too well: induces multiple ova, resulting in twins or greater multiple births |
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Term
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Definition
(SERM)
Agonist in non-breast tissue
Beneficial Effects
Bone
Liver
decreased total cholesterol, decreased LDL, no increase HDL
different than estrogen
Adverse Effects
Vasomotor
Increased risk of deep vein thrombosis, stroke
Can cause hot flashes
Endometrium (increased risk of uterine cancer)
was the first
Antagonist in breast
Used as treatment for breast cancer and as a prophylactic to prevent recurrence |
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Term
| Clomiphene, Tamoxifen, Raloxifene |
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Definition
Agents that act as estrogen receptor antagonists
BUT agents are not pure antagonists
Mechanism appears due to interactions with estrogen receptor accessory proteins in different tissues |
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Term
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Definition
Can be either combined synthetic estrogen + progestin or progestin only
Should be started as soon as possible after unprotected sex (99% effective if started within 72 hours)
Probable mechanisms to prevent pregnancy:
Prevention or delay of ovulation
Changed rate of tubal transport of ovum
Changes in the endometrium unfavorable to implantation
Induces nausea in 40%.
Sometimes given combined with anti-emetic
Progestin only version supposed to have less |
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Term
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Definition
Progesterone receptor antagonist (anti-progestin)
Causes endometrial shedding
Typically used in conjunction with a prostaglandin to induce uterine contractions
may be effective up to 50 days after |
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