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301 Cards in this Set
- Front
- Back
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Insulins & analogs
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Aspart
Detemir Glargine Glulisine Lispro NPH Regular crystalline insulin |
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Incretin-like drugs
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exenatide
sitagliptin |
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Amylin analogs
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pramlintide
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Sulfonureas
(oral anti-diabetic drugs) |
chlorpropamide
glipizide glyburide glimepiride tolbutamide |
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Meglitinides
(oral anti-diabetic drugs) |
Repaglinide
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Phenylalnine analogs
(oral anti-diabetic drugs) |
Nateglinide
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Biguanides
(oral anti-diabetic drugs) |
metformin
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Thiazolidinediones
(oral anti-diabetic drugs) |
Rosiglitazone
Pioglitazone |
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Alpha-glucosidase inhibitors
(oral anti-diabetic drugs) |
Acarbose
Miglitol |
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Rapid acting insulin
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lispro
aspart glulisine |
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Short acting insulin
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regular crystalline insulin
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Intermediate acting insulin
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NPH
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Long acting insulin
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detemir
glargine |
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Lispro
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Rapid acting insulin
modification of aa (B28 and B29) to Lys-Pro promotes adsorption by preventing self-association |
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Aspart
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Rapid acting insulin
Modification of aa (B28 pro to asp) promotes adsorption by preventing self association |
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Glulisine
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Rapid acting insulin
Modification of aa (B3 and B29 pro to lys and glu) promotes adsorption by preventing self association |
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Regular crystalline insulin
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Short acting insulin
wild type aa sequence |
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NPH
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Intermediate acting insulin
wild type aa sequence with protamine added in a 1:6 molar ratio cloudy solution with insulin complexed |
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Glargine
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Long-acting Insulin
modified aa (A21 to gly add two arg at B31 B32) insulin soluble at acidic pH, precipitates at neutral - slows absorption |
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Detemir
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Long-acting Insulin
modified aa (C-term B chain deleted, added myristic acid) increases self-aggregation and albumin binding |
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Chlorpropamide
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sulfonurea
first gen (less available) longest acting ~60 hrs increase insulin sec by decreasing K efflux reduce glucagon SDFX: hypoglycemia, resistance, weight gain |
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Tolbutamide
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sulfonurea
first gen (less available) increase insulin sec by decreasing K efflux reduce glucagon SDFX: hypoglycemia, resistance, weight gain |
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Glipizide
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sulfonurea
2d gen (more potent) increase insulin sec by decreasing K efflux reduce glucagon SDFX: hypoglycemia, resistance, weight gain |
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Glyburide
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sulfonurea
2d gen (more potent) increase insulin sec by decreasing K efflux reduce glucagon SDFX: hypoglycemia, resistance, weight gain |
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Glimepiride
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sulfonurea
2d gen (more potent) increase insulin sec by decreasing K efflux reduce glucagon SDFX: hypoglycemia, resistance, weight gain |
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Repaglintide
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meglitinide
bind ATP-K channels and increase insulin secretion with higher affinity than sulfonureas potent, 4-5 hour duration SDFX: hypoglycemia, wt gain, caution w/ renal or hepatic failure |
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Nateglinide
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D-phenylalanine analog
stimulates insulin secretion by blocking K channel faster, shorter action than meglitinides, with fewer SDFX safer for renal failure |
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Metformin
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biguanide
activate AMP kinase that senses energy changes, reduces hepatic glucose output SDFX: GI discomfort, lactic acidosis NO hypoglycemia |
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Rosiglitazone
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thiazolidinedione
agonist for PPAR-gamma, increase insulin sensitivity in target tissues SDFX: liver tox, CV, wt gain |
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Pioglitazone
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thiazolidinedione
agonist for PPAR-gamma, increase insulin sensitivity in target tissues SDFX: liver tox, CV, wt gain |
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Acarbose
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alpha-glucosidase inhibitor
reduces intestinal absorption of carbohydrates SDFX: flatulence, diarrhea, abdominal pain, hepatic tox? |
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Miglitol
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alpha-glucosidase inhibitor
reduces intestinal absorption of carbohydrates SDFX: flatulence, diarrhea, abdominal pain, hepatic tox? |
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Pramlintide
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amylin analog, SQ
inhibits glucagon secretion and has CNS mediated anorectic effect useful in both type I and II diabetics |
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Sitagliptin
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Inhibitor of incretin degredation
oral stimulates both beta and alpha cells (inc insulin, dec glucagon) decreasing postprandial glucose type II diabetics |
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Exenatide
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Incretin agonist
SQ stimulates both beta and alpha cells (inc insulin, dec glucagon) decreasing postprandial glucose type II diabetics |
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Thyroid hormones
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Thyroxine (T4)
Triiodothyronine (T3) T4+T3 |
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Thioamides/thiouracil
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Propylthiouracil
Methimazole |
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Other thyroid drugs
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Potassium iodide
Radioactive iodine |
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Misc agents for thyroid disease
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propranolol
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Propylthiouracil - PTU
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Thioamide
oral,works faster than MMI, less potent less risk to fetus than MMI, ok for lactation inhibit thyroidperoxidase initial timecourse is slow SDFX: skin rash, delayed hypothyroidism, agranulocytosis |
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Methimazole - MMI
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Thioamide
oral, more potent longer acting than PTU not pregnant, ok for lactation inhibit thyroidperoxidase initial timecourse is slow SDFX: skin rash, delayed hypothyroidism, agranulocytosis |
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Potassium iodide
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Iodide - greater than 6 mg / day
inhibits release and synthesis of T4 and T3 transient effect, fast acting SDFX: rash, swollen salivary glands |
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Radioactive iodine
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I-131, oral
concentrates in thyroid and damages it slow acting not pregnant/lactating SDFX: delayed hypothyroidism, radiation |
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Propranolol
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beta-adrenergic antagonist
used for symptoms of hyperthyroidism |
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Thyroxine
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T4 synthetic
t.5 7 days converted to T3 in peripheral tissues less expensive adverse: thyrotoxicosis, CV stress |
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Triiodothyronine
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T3 synthetic
4x as potent t.5 1 day more expensive adverse: thyrotoxicosis, CV stress |
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Glucocorticoids
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cortisol
dexamethasone prednisolone |
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Mineralocorticoids
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fludrocortisone
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Mineralocorticoid antagonists
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spironolactone
eplerenone |
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Synthesis inhibitors
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aminoglutethimide
metyrapone ketoconazole |
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Cortisol
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glucocorticoid
SDFX: hyperglycemia, myopathy, osteoporosis, cataracts, ulcers, behavior, ect... adrenal insufficiency on withdrawal |
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Prednisolone
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glucocorticoid
5:.3 (glucocorticoid to mineralocorticoid) SDFX: hyperglycemia, myopathy, osteoporosis, cataracts, ulcers, behavior, ect... adrenal insufficiency on withdrawal |
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Fludracortisone
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mineralocorticoid
10:250 (glucocorticoid to mineralocorticoid) useful for adrenal insufficency SDFX: fluid, electrolyte abnormalities, htn |
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Dexamethasone
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glucocorticoid
30:0 (glucocorticoid to mineralocorticoid) SDFX: hyperglycemia, myopathy, osteoporosis, cataracts, ulcers, behavior, ect... adrenal insufficiency on withdrawal |
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Spironolactone
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mineralocorticoid antagonist
also androgen antagonist used to treat primary aldosteronism |
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Eplerenone
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mineralocorticoid antagonist
not an androgen antagonist used to treat primary aldosteronism |
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Aminoglutethimide
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blocks adrenocortical steroid synthesis
inhibits conversion of cholesterol to pregnenolone treatment for Cushing's Syndrome |
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Metyrapone
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blocks adrenocortical steroid synthesis
inhibits conversion of 11-deoxy compounds to cortisol and corticosterone treatment for Cushing's Syndrome |
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Ketoconazole
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blocks adrenocortical steroid synthesis
inhibits many steps in steroid synthesis treatment for Cushing's Syndrome |
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Dexamethosone supression test
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Dexamethasone will supress cortisol if Cushing's is due to increased ACTH from pituitary, but not if there is primary adrenocortical hyperfunction or ACTH secretion by a tumor.
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estrogens
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estrodiol
ethinyl estrodiol estrone sulfate diethylstilbestrol |
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SERMs
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tamoxifen
raloxifene |
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Estrogen receptor antagonists
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clomiphene
ICI-182, 780 |
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Aromatase inhibitors
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Anastrozole
Exemestane |
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Progestins
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drospirenone
progesterone medroxyprogesterone acetate norethindrone norgestrel |
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Progestin receptor antagonists
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RU 486 (mifepristone)
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Gonadotropins
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FSH
CG |
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GnRH and analogs
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GnRH
synthetic agonist synthetic antagonist |
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Androgens
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testosterone
testosterone proprionate |
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17alpha-alkylated androgens
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methyltestosterone
danazol |
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5alpha-reductase inhibitors
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dutasteride
finasteride |
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Androgen receptor antagonists
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bicalutamide
flutamide nilutamide |
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progesterone
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Progestin
prevent fertilization by decreasing amount and viscosity of cervical mucus prevent ovulation by inhibiting hypothalamus and pituitary SDFX: headaches, abnormal bleeding |
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norethindrone
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Progestin
oral daily, IUD prevent fertilization by decreasing amount and viscosity of cervical mucus prevent ovulation by inhibiting hypothalamus and pituitary SDFX: headaches, abnormal bleeding |
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medroxyprogesterone acetate
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Progestin
IM 3 month injections prevent fertilization by decreasing amount and viscosity of cervical mucus prevent ovulation by inhibiting hypothalamus and pituitary SDFX: headaches, abnormal bleeding |
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norgestrel
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Progestin
oral daily prevent fertilization by decreasing amount and viscosity of cervical mucus prevent ovulation by inhibiting hypothalamus and pituitary SDFX: headaches, abnormal bleeding |
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Drospirenone
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Progestin
also has enhanced activity as mineralocorticoid and androgen antagonist prevent fertilization by decreasing amount and viscosity of cervical mucus prevent ovulation by inhibiting hypothalamus and pituitary SDFX: headaches, abnormal bleeding |
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estradiol
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estrogen
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ethinyl estradiol
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estrogen
combined with progestin (norethindrone or drospirenone) for oral contraceptive 21 on, 7 off, other patches, rings Prevent ovulation by inhibiting pituitary and hypothalamus (much more than progestin only), decrease cervical mucous to prevent fertilization SDFX: headaches, nausea, wt gain, CV in smokers decreased incidence of endometrial, ovarian cancer |
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diethylstilbesterol
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estrogen
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estrone sulfate
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estrogen
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Postcoital contraceptives
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high doses for a few days of est + prog or progestrin alone
90-98% effective if within 72 hours |
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clomiphene
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estrogen receptor antagonist
ant in bone, breast, CV system and uterus useful for induction of ovulation. When given in the early follicular phase, ant inhibitory effects of estrogen on pituitary and hypothalamus. (fertility Tx) |
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ICI-182, 780
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estrogen receptor antagonist
ant in bone, breast, CV system and uterus useful for induction of ovulation. When given in the early follicular phase, ant inhibitory effects of estrogen on pituitary and hypothalamus. (fertility Tx) |
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Tamoxifen
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Selective Estrogen Receptor Modulator
SERM agonist in bone, CV, uterus antagonist in breast useful for breast cancer, osteoporosis, post-menopausal symptoms |
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Raloxifene
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Selective Estrogen Receptor Modulator
SERM agonist in bone, CV antagonist in breast and uterus useful for breast cancer, osteoporosis, post-menopausal symptoms lower risk of thromboembolic events and uterine cancer than tamoxifen |
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anastrozole
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Aromatase inhibitor
non-steroidal inhibits conversion of testosterone to estradiol useful in breast cancer, ect... SDFX: hot flashes, lipids? |
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exemestane
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Aromatase inhibitor
steroidal inhibits conversion of testosterone to estradiol useful in breast cancer, ect... SDFX: hot flashes, lipids? |
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RU 486
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Progestin receptor antagonist
used for abortion with prostaglandin agonist also glucocorticoid agonist |
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testosterone
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androgen
transdermally or buccal tablets (not oral) replacement therapy in male hypogonadism treatment of some catabolic states (wasting) SDFX: feminization, suppression of hypothalamic-pituitary-gonadal axis, edema, jaundice, hepatic carcinoma |
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testosterone propionate
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androgen
replacement therapy in male hypogonadism treatment of some catabolic states (wasting) SDFX: feminization, suppression of hypothalamic-pituitary-gonadal axis, edema, jaundice, hepatic carcinoma |
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methyltestosterone
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17-alpha-alkylated androgen
more effective orally, more side effects (hepatic toxicity) than non-alkylated androgens uses: replacement therapy in male hypogonadism treatment of some catabolic states (wasting) SDFX: feminization, suppression of hypothalamic-pituitary-gonadal axis, edema, jaundice, hepatic carcinoma |
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danazol
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17-alpha-alkylated androgen
more effective orally, more side effects (hepatic toxicity) than non-alkylated androgens uses: replacement therapy in male hypogonadism treatment of some catabolic states (wasting) SDFX: feminization, suppression of hypothalamic-pituitary-gonadal axis, edema, jaundice, hepatic carcinoma |
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finasteride
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5alpha-reductase inhibitor
antiandrogen used for BPH, prost C, hirsutism, congenital adrenal hyperplasia... |
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dutasteride
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5alpha-reductase inhibitor
antiandrogen used for BPH, prost C, hirsutism, congenital adrenal hyperplasia... |
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flutamide
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androgen receptor antagonist
antiandrogen used for BPH, prost C, hirsutism, congenital adrenal hyperplasia... |
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bicalutamide
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androgen receptor antagonist
antiandrogen used for BPH, prost C, hirsutism, congenital adrenal hyperplasia... |
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nilutamide
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androgen receptor antagonist
antiandrogen used for BPH, prost C, hirsutism, congenital adrenal hyperplasia... |
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FSH
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gonadotropin
to induce follicular growth with LH to treat hypogonadotropic hypogonadism |
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CG
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gonadotropin
used to diagnose pregnancy to induce ovulation to treat cryptorchidism to treat hypogonadotropic hypogonadism |
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GnRH
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wild-type GnRH
injection used to stimulate GnRH secretion delayed puberty, anovulatory disorders |
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synthetic GnRH agonist
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long acting, after initial stimulation of gonadotropin secretion, supress it
used like GnRH antagonist to supress gonaotropin secretion |
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synthetic GnRH antagonist
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treatment of precocious puberty in boys and other androgen excesses
endometriosis and dysmenorrhea and stopping gonadotropin secretion in ovulation-induction |
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GH Related
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growth hormone
sermorelin acetate IGF-1 pegvisomant |
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Somatostatin agonists
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octreotide
lanreotide |
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D2 agonists
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bromocriptine
cabergoline pergolide |
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Posterior pituitary
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Desmopression
oxytocin vasopressin |
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Vitamin D & analogs
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vitamin D
vitamin D2 vitamin D3 |
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Miscellaneous calcium metabolism agents
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PTH
calcitonin |
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Bisphosphonates
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alendronate
etidronate pamidronate risedronate tiludronate |
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Growth Hormone
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human recombinant growth hormone, SQ, IM
used to stimulate growth in children correct metabolic problems in adults SDFX: mostly in adults, peripheral edema, carpal tunnel, impaired glucose tolerance, hypothyroidism children: increased intracranial pressure |
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Sermorelin acetate
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Synthetic GHRH analogue
SDFX: injection site reactions, headaches |
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IGF-1
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GH-related
human, recombinant used only in syndromes of GH resistance Only supplies growth effects, not metabolic |
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Pegvisomat
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GH-related
GH antagonist blocks the action of growth hormone (modified aa seq of wt GH complexed with polyethylene glycol) |
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Octreotide
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Somatostatin agonist
binds to type 2 and 5 receptors (not the ones n the pancreas) inhibits GH release SDFX: nausea, diarrhea, abdominal pain, gallstones |
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Lanreotide
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Somatostatin agonist
binds to type 2 and 5 receptors (not the ones n the pancreas) inhibits GH release SDFX: nausea, diarrhea, abdominal pain, gallstones |
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Bromocriptine
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D2 agonist
used to treat hyperprolactinemia (hypothalamic dopamine is an inhibitory factor for prolactin release) Tx: amenorrhea, infertility, galactorhea, preventing lactation SDFX: nausea, headaches, orthostatic hypotension |
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Cabergoline
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D2 agonist
used to treat hyperprolactinemia (hypothalamic dopamine is an inhibitory factor for prolactin release) Tx: amenorrhea, infertility, galactorhea, preventing lactation SDFX: nausea, headaches, orthostatic hypotension |
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Pergolide
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D2 agonist
used to treat hyperprolactinemia (hypothalamic dopamine is an inhibitory factor for prolactin release) Tx: amenorrhea, infertility, galactorhea, preventing lactation SDFX: nausea, headaches, orthostatic hypotension |
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Oxytocin
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Posterior pituitary hormone
modulates tm ion currents in myometrium for contractions used to induce labor |
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Vasopressin
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Posterior pituitary hormone
V1 receptors - vasoconstriction V2 receptors - renal tubule - increases water resorption used as replacement therapy in diabetes insipidus of pituitary origin |
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Desmopressin
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Posterior pituitary hormone
V1 receptors - vasoconstriction V2 receptors - renal tubule - increases water resorption used as replacement therapy in diabetes insipidus of pituitary origin |
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Vitamin D
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synthesized using liver, skin and kidney
causes increased adsorption of calcium (hypercalcemia) oral or IM |
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Vitamin D2
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(ergocalciferol)
causes increased adsorption of calcium (hypercalcemia) oral or IM |
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Vitamin D3
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(calcitriol)
causes increased adsorption of calcium (hypercalcemia) oral or IM |
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PTH
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parathyroid hormone
physiologically increases bone resorption at low and intermittent doses paradoxically increases bone formation Tx osteoporosis |
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Calcitonin
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Inhibits bone resorption and causes hypocalcemia
made in C cells of thyroid SQ, IM , nasal spray Salmon calcitonin and synthetic human calcitonin |
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Etidronate
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3-bisphosphonates
inhibit bone resorption - net hypocalcemia parenteral |
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Pamidronate
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3-bisphosphonates
inhibit bone resorption - net hypocalcemia parenteral |
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Alendronate
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3-bisphosphonates
inhibit bone resorption - net hypocalcemia parenteral or oral poorly absorbed orally, esopagitis |
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Risedronate
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3-bisphosphonates
inhibit bone resorption - net hypocalcemia parenteral or oral poorly absorbed orally, esopagitis |
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Tiludronate
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3-bisphosphonates
inhibit bone resorption - net hypocalcemia parenteral or oral poorly absorbed orally, esopagitis |
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Osteoporosis Tx
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exercise, no smoking
calcium, vitamin D prevent calcium mobilization: calcitonin, SERM, bisphosphanate, estrogen? stimulate bone formation: PTH- low & intermittant |
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Penicillins
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cell wall active agents
penicillin G penicillin V |
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Beta-lactamase resistant cell wall active agents
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oxacillin
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Extended spectrum cell wall active agents
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amoxicillin
ampicillin piperacillin ticarcillin |
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Beta lactamase inhibitors
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clavulanic acid
sulbactam tazobactam |
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Cephalosporins
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cell wall active agents
1st gen cephalexin cefazolin 2d gen cefaclor 3d gen cefixime 4th gen cefepime |
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Carbapenems
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cell wall active agents
imipenem meropenem cilastatin - peptidase inhibitor |
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Monobactams
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cell wall active agents
aztreonam |
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Other cell wall active agents
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Bacitracin
daptomycin fosfomycin vancomycin |
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Penicillin G
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beta-lactams inhibit transpeptidase, bactericidal, exr in urine, not topical, not to CNS
oldest penicillin - G+/G- cocci oral not very effective - IV different salts lactamase sensitive |
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Penicillin V
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beta-lactams inhibit transpeptidase, bactericidal, exr in urine, not topical, not to CNS
orally absorbed better than penicillin G, similar oral not suitable for serious infections |
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Oxacillin
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beta lactamase resistant beta-lactam inhibit transpeptidase, bactericidal, exr in urine, not topical, not to CNS
penicillinase resistant staph, mixed staph and strep infections more side effects (enterococci and MRSA resistant) |
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Amoxicillin
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Extended spectrum penicillin
non-lactamase g- bacilli (E coli, salmonella, shigella, H. influenzae.) |
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Ampicillin
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Extended spectrum penicillin
like amoxicillin Tx: non-lactamase g- bacilli (E coli, salmonella, shigella, H. influenzae.) often rashes, oral absorption reduced by food |
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Piperacillin
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Extended spectrum penicillin
carbenacillin-like not lactamase resistant parenteral reserved for serious infection - pseudomonas |
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Ticarcillin
|
Extended spectrum penicillin
carbenacillin-like not lactamase resistant parenteral reserved for serious infection - pseudomonas |
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clavulanic acid
|
beta lacatmase inhibitor
suicide substrate stops lactamse synergistic when used with amoxicillin to treat beta-lactamase producers |
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sulbactam
|
beta lacatmase inhibitor
suicide substrate stops lactamse synergistic when used with amoxicillin to treat beta-lactamase producers |
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tazobactam
|
beta lacatmase inhibitor
suicide substrate stops lactamse synergistic when used with amoxicillin to treat beta-lactamase producers |
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Cephalexin
|
Cephalosporin -1st GEN
g+, some ca g-, not CNS surgical prophylaxis, staph & strep inhibitor of cell wall synthesis not topical oral, IV, IM, excr in urine SDFX: well tol, GI, allergy 5% |
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Cefazolin
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Cephalosporin -1st GEN
g+, some ca g-, not CNS surgical prophylaxis, staph & strep inhibitor of cell wall synthesis not topical oral, IV, IM, excr in urine SDFX: well tol, GI, allergy 5% |
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Cefaclor
|
Cephalosporin 2d GEN
g+, extended g-, some efficacy vs oral and bowel anaerobes inhibitor of cell wall synthesis not topical oral, IV, IM, excr in urine SDFX: well tol, GI, allergy 5% |
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Cefixime
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Cephalosporin -3d GEN
g+, extended g-, penetrates CNS! use for meningitis inhibitor of cell wall synthesis not topical oral, IV, IM, excr in urine SDFX: well tol, GI, allergy 5% |
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Cefepime
|
Cephalosporin -4th GEN
g+, extended g-, enhanced betalactamse resistance penetrates CNS! use for meningitis as good as 1st gen for g+ (unlike 2&3 gen) inhibitor of cell wall synthesis not topical oral, IV, IM, excr in urine SDFX: well tol, GI, allergy 5% |
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Imipenem
|
Carbapenem
like penicillin- C instead of S g+, g- rods, anaerobes - Tx serious nosocomial infections resistant to many beta lactamses parenteral. renal excr., crosses CNS coadminister with renal dehydropeptidase inhibitor (cilastatin) SDFX: neurotox, seiz, GI, cross allergy w/pen |
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Meropenem
|
Carbapenem- doesn't need cilastatin
like penicillin- C instead of S g+, g- rods, anaerobes - Tx serious nosocomial infections resistant to many beta lactamses parenteral. renal excr., crosses CNS SDFX: neurotox, seiz, GI, cross allergy w/pen |
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Cilastatin
|
renal dehydropeptidase inhibitor coadminister with meropenem
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Aztreonam
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Monobactam
g- rods, no g+ or anaerobes (like aminoglycasides, less toxic) same mech as penicillin, synthetic IM/IV, renal elim, ent. inflamed CNS SDFX: mild, phlebitis at inj |
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Vancomycin
|
inh cell wall synthesis by blocking precursor formation
g+ cocci, bacilli, not many g- MRSA, coag-staph, strep pneumo, combo w/aminoglycocides synergy bactericidal for dividing cultures excr kidney, not oral (except for gut), CNS if infl SDFX:hypersens, phlebitis, ototox/nephrotox at high dose |
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Bacitracin
|
Interferes with cell wall biosynthesis
nephrotoxicity limits to topical admin oral for gut (poorly absorbed) hypersensitivity rare |
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Daptomycin
|
depolarizes g+ bacteria, rapidly bacteriocidal
MRSA, Strep, vanc resistant enterococcus new, novel IV, renal exc SDFX: muscle pain/weakness, incr creatine phosphokinase |
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Fosfomycin
|
inh cell wall biosynthesis by blocking peptidoglycan synthesis
SINGLE dose uncomplicated UTI's exr. unchanged into urine |
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Aminoglycosides
|
amikacin
gentamicin neomycin tobramycin |
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Tetracyclines
|
tetracycline
doxycycline |
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Macrolides
|
azithromycin
clarithromycin erythromycin telithromycin |
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Lincomycins
|
clindamycin
|
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Streptogramins
|
quinupristin
dalfopristin |
|
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Misc agents that inhibit bacterial protein synthesis
|
chloramphenicol
linezolid mupirocin |
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Gentamicin
|
Aminoglycoside
IM, slow IV resistant aerobic g- (e coli, kleb, pseudomonas) SDFX: low TI, ototox.nephrotoxicity bind to 30s bacterial ribosomal subunit blocks initiation, translation, causes wrong aa insertion -rapidly bacteriocidal excluded from cells, low CNS, poor oral absorp, renal excr |
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Neomycin
|
Aminoglycoside
IM, slow IV, oral for GI preop resistant aerobic g- (e coli, kleb, pseudomonas) SDFX: low TI, ototox.nephrotoxicity bind to 30s bacterial ribosomal subunit blocks initiation, translation, causes wrong aa insertion -rapidly bacteriocidal excluded from cells, low CNS, poor oral absorp, renal excr |
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Tobramycin
|
Aminoglycoside
IM, slow IV resistant aerobic g- (e coli, kleb, pseudomonas) SDFX: low TI, ototox.nephrotoxicity bind to 30s bacterial ribosomal subunit blocks initiation, translation, causes wrong aa insertion -rapidly bacteriocidal excluded from cells, low CNS, poor oral absorp, renal excr |
|
|
Amikacin
|
Aminoglycoside
IM, slow IV resistant aerobic g- (e coli, kleb, pseudomonas) SDFX: low TI, ototox.nephrotoxicity bind to 30s bacterial ribosomal subunit blocks initiation, translation, causes wrong aa insertion -rapidly bacteriocidal excluded from cells, low CNS, poor oral absorp, renal excr |
|
|
tetracycline
|
tetracycline
g+, g-, amoeba DOC lyme, RMSF, mycoplasma, chlamydia bacteriostatic- inhibits protein synthesis by binding bacterial 30s incomplete gut uptake - decr w/ antacids/milk crosses BBB, placenta, milk hepatic metabolization - induced by barbs/phenytoin, increases warfarin effect SDFX: GI, phootsensitivity, teeth discoloration, yeast superinfection |
|
|
doxycycline
|
tetracycline
g+, g-, amoeba DOC lyme, RMSF, mycoplasma, chlamydia bacteriostatic- inhibits protein synthesis by binding bacterial 30s incomplete gut uptake - decr w/ antacids/milk crosses BBB, placenta, milk hepatic metabolization - induced by barbs/phenytoin, increases warfarin effect SDFX: GI, phootsensitivity, teeth discoloration, yeast superinfection |
|
|
Chloramphenicol
|
misc protein synthesis inhibitor
toxic, severe infections, broad spectrum bacteriostatic, inhibits transpeptidase rxn binds to bacterial 50S crosses BBB, placenta, milk hepatic metabolism (inhibits p450), renal excretion SDFX: anemia, leukopenia, thrombocytopenia, aplastic anemia, gray baby partial inhibition of eukaryotic & Mt protein synth |
|
|
erythromycin
|
macrolide
g-, g+ aerobes, some anaerobes mycoplasma, pertussis, diptheriae inhibits translocation by binding to bacterial 50S, bacteriostatic oral/IV enters cells, no CNS enteric coating-hydrolyzed in stomach concentrated in liver, excreted in bile SDFX: very safe, GI, jaundice, drug interactions |
|
|
azithromycin
|
macrolide
broader spectrum, oral avail. than erythromycin STDs (longer half-life) g-, g+ aerobes, some anaerobes mycoplasma, pertussis, diptheriae inhibits translocation by binding to bacterial 50S, bacteriostatic oral/IV enters cells, no CNS concentrated in liver, excreted in bile SDFX: very safe, GI, jaundice, drug interactions |
|
|
clarithromycin
|
macrolide
broader spectrum, oral avail. than erythromycin g-, g+ aerobes, some anaerobes mycoplasma, pertussis, diptheriae inhibits translocation by binding to bacterial 50S, bacteriostatic oral/IV enters cells, no CNS concentrated in liver, excreted in bile SDFX: very safe, GI, jaundice, drug interactions |
|
|
telithromycin
|
macrolide
semisynthetic erythromycin derivitave - more stable, less resistance CA respiratory infections, sinusitis, bronchitis inhibits translocation by binding to bacterial 50S, bacteriostatic renal & hepatic elimination SDFX: GI, vision, exacerbation of myasthenia gravis, drug int w/ simvastatin |
|
|
Clindamycin
|
Lincomycin
binds to 50s - bacteriostatic -novel structure oral/IV/IM no CNS Tx: bacteroides f., penicillin allergic/resistant hepatic/biliary excretion - stays in gut SDFX: pseudomembranous colitis, skin rashs |
|
|
Dalfopristin
|
streptogramin
binds 50s bacteriostatic alone, cidal w/ Quinupristin Tx: VR enterococcus faececium parenteral, hepatic met, renal.biliary exr SDFX: inflammation at inj site, GI, drug interactions w/HIW drugs, cyclosporine, Ca channel blockers |
|
|
Quinupristin
|
streptogramin
binds 50s bacteriostatic alone, cidal w/ Dalfopristin Tx: VR enterococcus faececium parenteral, hepatic met, renal.biliary exr SDFX: inflammation at inj site, GI, drug interactions w/HIW drugs, cyclosporine, Ca channel blockers |
|
|
Linezolid
|
Misc inhibitor of bacterial protein synthesis
no cross resistance - novel ribosomal binding Tx: VREF, multiple drug resistant infectins oral availability, hepatic metabolism, renal excretion SDFX: GI, mild thrombocytopenia |
|
|
Mupirocin
|
Misc inhibitor of bacterial protein synthesis
topically bacteriocidal - rapidly inactivated if sysytemic Tx: impetigo of S. aureus, S. pyogenes SDFX: only allergic |
|
|
Iron
|
ferrous fumarate
ferrous gluconate ferrous sulfate |
|
|
Chelators
|
deferasirox
desferoxamine |
|
|
Vitamins used in anemia
|
B-12
|
|
|
Hematopoietic growth factors
|
erythropoietin
G-CSF GM-CSF |
|
|
Oral iron replacement
|
ferrous salts (sulfate, gluconate, fumarate)
NOT enteric coated, absorption in early intestine 3-6 months for repletion SDFX: cramps, nausea, constipation, diarrhea, heme - black stools |
|
|
deferasirox
|
chelator (iron toxicity)
oral fecal excretion of iron headache, renal toxicty |
|
|
desferoxamine
|
chelator (iron toxicity)
parenteral fecal and urinary excretion of iron ototoxicity, ocular toxicity |
|
|
Vitamin B12
|
pernicious anemia
lack of intrinsic factor, small bowel problems anemia (helps recycle folate), fatigue, sore tongue, neurological symptoms |
|
|
Erythropoietin
|
hematopoietic growth factor
stimulates proliferation & maturation of commited erythrocyte progentors (CFU-E) acts synergistically with IL-3 and GM-CSF to expand BFU-E compartment stimulates early release of reticulocytes SDFX: Htn, seizures |
|
|
G-CSF
|
hematopoietic growth factor
stimulates granulocyte colonies and PMN production, release of granulocytes |
|
|
GM-CSF
|
hematopoietic growth factor
with IL-3 stimulates colonies and prolif of granulocytes, mono/mac, and megakaryocytes |
|
|
Sulfonamides
|
sulfanilamide
sulfamethoxazole |
|
|
DHFR inhibitors
|
trimethoprim
tmp-sulfa |
|
|
fluoroquinalones
|
ciprofloxacin
levofloxacin moxifloxacin |
|
|
sulfanilamide
|
sulfanamide
bacteriostatic, inhibit synthesis of dihydrofolic acid (and thus DNA synthesis) Tx: broad spec g+/g-/parasites plasmodium and toxoplasma resistance is common oral/IV, +CSF, met by liver, excr kidney SDFX: common, GI, rash, bone marrow, liver, kernicterus in infants, G6PD hemolytic anemia, Stevens Johnson S |
|
|
sulfamethoxazole
|
sulfanamide
bacteriostatic, inhibit synthesis of dihydrofolic acid (and thus DNA synthesis) Tx: broad spec g+/g-/parasites plasmodium and toxoplasma resistance is common oral/IV, +CSF, met by liver, excr kidney SDFX: common, GI, rash, bone marrow, liver, kernicterus in infants, G6PD hemolytic anemia, Stevens Johnson S |
|
|
Trimethoprim
|
DHFR inhibitor
acts sequentially in purine synthesis synergistic w/sulfa - combo bacteriocidal |
|
|
tmp-sulfa
|
sulfanilamide & DHFR inhibitor
combo bacteriocidal oral, renal excretion Tx: caMRSA, UTIs, pneumocystis g+,g- not pseudomonas, not amaerobes/atypical SDFX: common, GI, rash, neutropenia & bone marrow, liver, kernicterus in infants, |
|
|
ciprofloxacin
|
fluoroquinolone
inhibits DNA gyrase, topoisomerase Tx: UTIs, STDs, pneumonia g-, pseudomonas cipro>levo>moxi g+, moxi>levo>cipro atypicals (eg mycoplasma) not anaerobes bacteriocidal, [] dependant good GI absorption, no synergy SDFX: GI, achilles tendon, Qt |
|
|
levofloxacin
|
fluoroquinolone
inhibits DNA gyrase, topoisomerase Tx: UTIs, STDs, pneumonia g-, pseudomonas cipro>levo>moxi g+, moxi>levo>cipro atypicals (eg mycoplasma) not anaerobes bacteriocidal, [] dependant good GI absorption, no synergy SDFX: GI, achilles tendon, Qt |
|
|
moxifloxacin
|
fluoroquinolone
inhibits DNA gyrase, topoisomerase Tx: UTIs, STDs, pneumonia g-, pseudomonas cipro>levo>moxi g+, moxi>levo>cipro atypicals (eg mycoplasma) not anaerobes bacteriocidal, [] dependant good GI absorption, no synergy SDFX: GI, achilles tendon, Qt |
|
|
inhibitor of viral penetration
|
amantadine
rimantidine enfurtidine maraviroc |
|
|
inhibitor of viral nucleic acid synthesis
|
ribavarin
|
|
|
polymerase/RT inhibitors
|
foscarnet
|
|
|
neuraminidase inhibitors
|
oseltamivir
zanamivir |
|
|
nucleoside analogs
|
acyclovir
ganciclovir famciclovir idoxuridine vidarabine |
|
|
reverse transcriptase inhibitors
|
AZT
efavirenz nevirapine |
|
|
protease inhibitors
|
indinavir
ritonavir |
|
|
HIV fusion inhibitor
|
enfuvirtide
|
|
|
HIV integrase inhibitor
|
raltegravir
|
|
|
CCR5 co-receptor antagonist
|
maraviroc
|
|
|
amantidine
|
inhibitor of viral penetration
Tx: influenza A and Rubella prophylaxis 70% effective, tx after infection reduces symptoms oral absorption, renal excretion SDFX: insomnia, CNS symptoms |
|
|
rimantadine
|
inhibitor of viral penetration
Tx: influenza A and Rubella prophylaxis 70% effective, tx after infection reduces symptoms oral absorption, renal excretion SDFX: insomnia, rimant has fewer CNS symptoms |
|
|
enfurtidine
|
inhibitor of viral penetration
Tx: influenza A and Rubella prophylaxis 70% effective, tx after infection reduces symptoms oral absorption, renal excretion SDFX: insomnia, CNS symptoms |
|
|
|
|
|
|
Ribavirin
|
Inhibitor of viral nucleic acid synthesis
inhibits GMP accumulation Tx:RSV, influenza A, B, Lassa shortens course pregnancy category X |
|
|
Foscarnet
|
Polymerase/RT inhibitor
Tx: CMV retinitis, HSV, VZV IV only, +CNS kidney excretion, incorp into bone SDFX: renal, naus/vom |
|
|
Oseltamivir
|
Neuraminidase inhibitor
Tx: influenza A&B prophylaxis, acute in pts w/ <2 days symptoms oral, prodrug, renal excretion SDFX: naus/vom, rare stevens-johnson |
|
|
Zanamivir
|
Neuraminidase inhibitor
Tx: influenza A&B prophylaxis, acute in pts w/ <2 days symptoms oral, prodrug, renal excretion SDFX: naus/vom, rare stevens-johnson |
|
|
Acyclovir
|
nucleoside analog (G)
oral 15-20% availability, IV HSV and HZV, transplant patients SDFX: well tolerated |
|
|
Famciclovir
|
nucleoside analog
oral 15-20% availability HSV-2 and HZV SDFX: well tolerated |
|
|
Vidarabine
|
nucleoside analog (A)
IV for severe herpes infection (after acyclovir) SDFX: GI, mild CNS |
|
|
Idoxuridine
|
nucleoside analog (T)
inhibits viral (also some host) DNA synth herpatic keratitis of the cornea |
|
|
Ganciclovir
|
nucleoside analog (G)
preferentially phosphorylated by CMV i-c CMV infections IV, penetrates BBB SDFX: leukopenia, neutropenia, throbocytopenia, renal toxicity |
|
|
AZT
|
Nucleoside analog RT inhibitor (NRTI)
oral, + CNS, rapid excr, hep met Tx: HIV in combo therapy, monotherapy to prevent maternal-neonate HIV spread SDFX: bone marrow, granulocytopenia, thrombocytopenia, headaches, rash, fever, diarrhea |
|
|
Nevirapine
|
Non-nucleoside analog RT inhibitor (NNRTI)
binds to RT Tx: combo HIV therapy, reduce maternal-fetal transmission +CNS, hep CYP450, kidney excr SDFX: severe skin, hepatotoxicty, drug interactions |
|
|
Efavirenz
|
Non-nucleoside analog RT inhibitor (NNRTI)
binds to RT Tx: combo HIV therapy, reduce maternal-fetal transmission +CNS, hep CYP450, kidney excr SDFX: severe skin, hepatotoxicty, drug interactions |
|
|
Indinavir
|
protease inhibitor
Tx: HIV HAART |
|
|
Ritonavir
|
protease inhibitor
Tx: HIV HAART |
|
|
Enfuvirtide
|
HIV fusion inhibitor
reserved for "treatment experienced pts" 36 aa synthetic peptide binds to pg41 of HIV-1, prevents fusion SQ BID, met/elim? SDFX: injection site reactions, pneumonia, hypersensitivity |
|
|
Raltegravir
|
HIV integrase inhibitor
inhibits activity of HIV-1 integrase Tx: resistant HIV-1 oral, met in liver, excr in urine SDFX:headache, nausea, fatigue, myopathy, rhabdomyolysis, interacts with rifampin |
|
|
Maraviroc
|
CCR5-coreceptor antagonist - inhibits viral penetration
Tx: CCR5-tropic strains of HIV-1 (reserved for resistant pts) oral, CYP3A metabolism (conc increased by protease inhibitors) SDFX: hepatotoxicity, rash, musculoskelatal |
|
|
polyenes
|
target fungal cell membrane
amphotericin B nystatin |
|
|
azoles
|
target fungal cell membrane
imidazoles: clotrimazole ketoconazole miconazole triazoles: fluconazole voriconazole |
|
|
allylamines
|
target fungal cell membrane
terbinafine |
|
|
Echinocandins
|
target fungal cell wall
caspofungan |
|
|
DNA synthesis antimetabolite (antifungal)
|
flucytosine
|
|
|
mitotic spindle antifungal
|
griseofulvin
|
|
|
misc antifungal
|
tolnaftate
|
|
|
Superficial fungal infections
|
nystatin
griseofulvin miconazole and clotrimazole terbinafine |
|
|
Systemic fungal infections
|
amphoteracin B
flucytosine ketoconazole fluconazole |
|
|
Amphotericin B
|
polyene binds ergosterol in fungal cell membrane
tx: life-threatening systemic infections slow IV - >90% bound to plasma p's doesn't x BBB, intrathecal injection SDFX: fever, aches, GI, nephrotox, anemia, thrombopenia, leukopenia unstable - complexed or lipid formulations |
|
|
Flucytosine
|
Pyrimidine analog- inhibits fungal DNA synthesis
Tx: candida, cryptococcal, used with amphotericin B or triazole enters CNS, renal excretion unchanged don't use with renal insufficiency SDFX: naus/vom, rash, leukopenia, thrombocytopenia |
|
|
Ketoconazole
|
synthetic imidazole
targets fungal cell membrane by inhibiting ergosterol synthesis Tx: chronic candidiasis, paracoccidiomycosis (not 1st choice for any) oral w/ food, avoid antacids hepatic degradation SDFX: naus/vom, rash, hepatotox, gynecomastia, drug interactions |
|
|
Fluconazole
|
triazole (less effect on host that imidazoles)
fungistatic inhibition of ergosterol synthesis Tx: oropharyngeal and esophageal candidiasis oral, +CNS, urine excretion unchanged SDFX: well tolerated, GI, rare thrombocytopenia |
|
|
Voriconazole
|
triazole (less effect on host that imidazoles)
fungistatic inhibition of ergosterol synthesis Tx: oropharyngeal and esophageal candidiasis oral, +CNS, urine excretion unchanged SDFX: well tolerated, GI, rare thrombocytopenia |
|
|
Terbinaphine
|
allylamine - inhibits squalene epoxidase (ergosterol pathway) - fungal cell membrane
Tx: onchomycosis of toanil/fingernail, topical skin candida, trichophyton oral, topical, hepatic met, renal elim (red in liver&kidney failure) SDFX: GI, skin, liver |
|
|
Caspofungin
|
echinocandin - targets fungal cell wall (beta 1,3-D-glucan synthase)
fungicidal Tx: IV only, candidemia, aspergillosis renal and hepatic elimination, adj dose for hepatic insufficiency SDFX: histamine mediated, less than amphotericin B |
|
|
Griseofulvin
|
inhibits fungal mitotic spindle
fungicidal for dividing cells Tx: NOT candida, microsporum, epidermophyton, trichopytn oral, aided by high fat foods, long Tx, binds keratin, not topical, inactivated in liver, slowly excr in urine SDFX: induces p450s, GI, penicillin Xreactions |
|
|
Nystatin
|
polyene targets fungal cell membrane
TOPICAL, not oral, not IV Tx: candidia infections of skin, mucous, bowel |
|
|
Clotrimazole
|
synthetic imidazole
targets fungal cell membrane by inhibiting ergosterol synthesis Tx: oral, vaginal, cutaneous candidiasis TOPICAL, not oral, not IV |
|
|
Miconazole
|
synthetic imidazole
targets fungal cell membrane by inhibiting ergosterol synthesis Tx: oral, vaginal, cutaneous candidiasis TOPICAL, not oral, not IV |
|
|
first line anti-tuberculosis
|
ethambutol
isoniazid pyrazinamide rifampin |
|
|
second line anti-tuberculosis
|
ciprofloxacin
cycloserine ethionamide p-amino salicylic acid streptomycin |
|
|
anti-M. avium complex
|
Rifabutin
|
|
|
Anti-leprosy
|
dapsone
rifampin |
|
|
Isoniazid
|
1st line anti-tuberculosis
inhibits mycolic acid biosynthesis prevention, part of multi therapy bacteriostatic, cidal for dividing cells oral, parenteral, in cells, CNS, excr urine hepatic insuff ->elevated levels SDFX: rash, fever, jaundice, peripheral neuritis |
|
|
Rifampin
|
1st line anti-tuberculosis
inhibits bacterial RNA pol oral (food hinders), bile-enterohepatic elim, +CNS SDFX: rash,fever, naus/vom, jaundice, induces liver enzymes |
|
|
Ethambutol
|
1st line anti-tuberculosis
inhibits mycolic acid integration into cell wall, bacteriostatic only for dividing bacteria oral, urine excr unchanged (accumulates in renal impaired) SDFX: milder, vision, rash, fever, rare CNS, pruritis, red-green colorblindness |
|
|
Streptomycin
|
2d line anti-tuberculosis
drug resistance limits usefulness |
|
|
Pyrazinamide
|
1st line anti-tuberculosis
bacteriocidal - unknown mechanism oral, hydrolyzed and excr by kidney SDFX: hepatotoxicity, GI effects |
|
|
Ciprofloxacin
|
2d line anti-tuberculosis
inhibits gyrase and topoisomerase bacteriocidal oral, uptake reduced with antacids SDFX: skin, photosensitivity, GI |
|
|
M.tb combination therapy
|
often
Isoniazid, Rifampin, Pyrazinamide, (ethambutol or streptomycin), 6-18 months |
|
|
Mycobacterium avium
|
common in AIDS patients, doesn't respon to most anti-mycobacterials
rifabutin used, macrolides, quinalones in combination |
|
|
Leprosy
|
mycobacterium leprae
combination therapy including dapsone rifampin |
|
|
CYP34A
|
metabolizes ~50% drugs
expression increased by inducers: rifampin, carbamazepime, phenobarbital, phenytoin, St/ John's Wort Inhibited by: cimetadine, erythromycin, ketoconazole |
|
|
CYP2D6
|
metabolizes ~25% drugs
anti-depressents,, anti-psychotics, beta blockers ultra rapid and poor metabolizers |
|
|
CYP2C9
|
metabolizes Warfarin
some patients are poor metabolizers (toxicity) |
|
|
CYP2C19
|
metabolizes carisoprodol and diazepam
|
|
|
UGT1A1
|
gluconuridation of bilirubin
deficiency can cause irinotecan toxicity |
|
|
TPMT
|
thiopurine methyltransferase
transforms azathrioprine and 6-mercaptopurine |
|
|
VKORC1
|
vitamin K epoxide reductase complex 1
targeted by Warfarin |
|
|
Air pollutants
|
carbon monoxide
nitrogen dioxide ozone sulfur dioxide |
|
|
Alcohols
|
ethenol
ethylene glycol isopropanol methanol |
|
|
Inhibitors of alcohol metabolism
|
4-methylpyrazole
disulfiram |
|
|
Heavy metals
|
Arsenic
Cadmium Lead Mercury |
|
|
Chelators
|
dimercaprol
penicillamine |
|
|
POPs
|
cyclodienes: dieldrin, chlordane, toxaphene
halogenated industials: polychlorinated biphenyls (PCBs) Brominated flame retardants: polybrominated diphenyl esters (PBDEs) |
|
|
Carbon monoxide
|
air pollutant
incomplete combustion 2-31% mortality winter: car exhaust, fire, smoking fetal hemoglobin binds CO more avidly than adult if survive, long-term CNS/CV toxicity |
|
|
Sulfur Dioxide
|
air pollutant
coal combustion water soluble, upper airway damage toxicity severe in asthma, COPD, emphysema |
|
|
Nitrogen Oxides
|
air pollutant
power plants and cars NO2 brownish, highly reactive penetrates deep in lung potent respiratory toxin |
|
|
Ozone
|
air pollutant
photochemical reaction (NOx cycle) reactive: peroxidizes lipids, oxidixes thiols, amines, proteins deep in lung respiratory damage, asthma, bronchitis,.... |
|
|
Ethanol
|
metabolized by ADH (alcohol dehydrogenase) to acetaldehyde (zero order kinetics), aspirin inhibits ADH
small amount by p450 and catalase |
|
|
Disulfiram
|
Anabuse
aldehyde dehydroginase inhibitor used in alcohol abuse treatment |
|
|
4-methyl pyrazole
|
alcohol dehydrogenase (ADH) inhibitor
used in alcohol abuse |
|
|
Isopropanol
|
antiseptic and disinfectant
rapid GI absorption, metabolism to acetone, slow elimination in kidneys and lung resp depressant, renal dysfunction do not use EtOH as antidote |
|
|
Methanol
|
solvent, GI, skin, lung absorption
elimination hepatic to formaldehyde and formic acid highly toxic CNS, ocular, GI, acidosis EtOH as antidote as part of Tx |
|
|
Ethylene Glycol
|
antifreeze
GI absorption, renal filtration metabolized to glycoaldehyde, glycolic acid, oxalic acid low affinity to ADH comp to EtOH CNS depression, CV, acidosis, renal toxicity, renal failure EtOH as antidote |
|
|
Arsenic
|
binds to sulfhydryl groups in hair and nails
toxicity in GI, renla, skin, CV, CNS accumulates in Mt, inhibots -SH enzymes acute: large dose lethal, chleation chronic: lots of systems, cancer chelation |
|
|
Cadmium
|
trace element, divalent, bioaccumulation
food, smoking, occupationl liver & kidneys acute: oral -naus/vom, death. inhalation - pneumonitis, p edema, death no good Tx chronic: COPD, bronchitis, emphysema, systolic Htn, bone pain, osteomalacia cancer |
|
|
Lead
|
food, environment, recreation, paint
oral uptake better in kids, inhalation, RBCs storage in skeleton, soft tissue (esp brain in kids) excretion urine, milk, fetus acute: GI, encepalopathy, nephropathy, developmental Chronic: neuropathy, gout, anemia, CNS, cancers Tx: chelation therapy, but mobilizes bone Pb, rebound effect |
|
|
Mercury
|
elemental, inorganic (ic or ous), organic
CNS damage, Kidney damage, CV damage, prenatal severe damage |
|
|
Cyclodienes
|
POPs - halogenated insecticides
dieldrin chlordane toxaphene stimulate CNS, GABA antagonists GI, carcinogenic, Lethality |
|
|
Halogenated industrial compounds
|
POPs
PCBs =polychlorinated biphenyls food, air from products Skin, respiratory syndrome, GI, hormone disruption, immunosupression, reproductive, developmental, cancer |
|
|
Brominated Flame Retardants
|
POPs
PBDEs = polybrominated diphenyl esters toxic effects in humans not yet known carcinogen? endocrine? (rats) air, dust, food, ubiquitous |
