Pharm: Focus Drug List MOA and AE: Cook Flashcards
Acarbose
a-glucosidase inhibitor:
- -reduce intestinal disaccharide/starch absorption
- -reduce post-eating glucose elevation
- -not used alone
Use:
DM2
AE:
-Terrible gas…
Alendronate
Ibandronate
Risedronate
Zoledronic acid (Zonedronate)
Bisphosphonates:
- non-hydrolyzable analog of pyrophosphate swallowed up by osteoclasts who die
- inhibit bone resorption
Use:
Paget’s
Osteoporosis
AE:
- Esophageal/GI ulcers (no food 30 min, sit upright)
- Osteonecrosis of jaw
Breakdown of bisphosphonate potency?
10-100x: 2nd gen
Alendronate
Ibandronate
1k-10k x: 3rd Gen
Risendronate
Zonendronate/Zolendronic AcidWho do you give 3rd generation bisphosphonates to?
Cancer patients: Maybe 1 dose to stop bone resorption by mets. IV only!
- Risendronate
- Zonendronate
Hydrocortisone Prednisolone/Prednisone Methylprednisolone Betamethasone Dexamethasone
Cortisol:
- Bind GCRs to modify transcription of GREs
- Inhibit: NFkB, AP-1, NFAT, Phospholipase A2
- Decrease: TNFa, IL1, IL6; (PLP: decrease LT, PGs)
Use: Adrenal removal, inflammation, etc…
AE: WEAN OFF!!!!! due to pituitary atrophy Osteoporosis DM Peptic ulcers CNS: euphoria Men: Hypogonadism (pit. decrease) Women: Dyrhythmic cycles, bleeding Kids: GH inhibition, IGF1 decrease, decrease growth
What is the potency of Hydrocortisone?
1x
Short acting
Cortisol equivolent
Oral/IV/IM
What is the potency of prednisolone/prednisone?
4x
Short acting
0.3Na–>swelling
Oral ONLY
What is the potency of methylprednisolone?
5x
Short acting
0.5 Na–>swelling
ALLERGIES?
What is the potency of betamethasone?
25-40x
Powerful
Oral/Topical
What is the potency of dexamethasone?
30x
All administrations
EYE disease
What class of glucocorticoids have mineralocorticoid action?
Short acting: prednisolone/methyl
Capergoline
Bromocriptine
Capergoline: D2 Dopamine agonist
Bromocriptine: poorly tolerated D2 agonist
Calcipotriol
PSORIASIS Vit D!
Vit D derivative for calcium regulation, stimulates Ca and Phos. absorption in GI
Used for psoriasis, hypoparathyroidism, osteoporosis.
More effective than glucocorticoids for psoriasis?
Calcitriol
Active 1,25 D3
Made in skin–>liver–>kidney
Vit D derivative for calcium regulation, stimulates Ca and Phos. absorption in GI
Calcium supplements
Increase calcium in hypocalcemia
Cetrorilix
Ganirelix
GnRH receptor antagonist:
-Block GnRH to delay LH surge and ovulation for in vitro ovulation.
Degarelix
GnRH receptor antagonist for prostate cancer LH reduction.
Menotropin
LH/FSH purification for infertility.
IM injection.
Octreotide
Somatostatin analog:
Block GH, Insulin, Glucagon
Goserelin
GnRH agonist for prostate cancer, give high dose to cause chemical castration and prevent T release.
Levothyroxine (synthroid)
L-T4.
Higher doses required in kids.
Can take weeks for steady state.
Monitor T3/T4 closely: narrow TI
Liothyronine sodium
L-T3
Tablets or injection
Propylthiouracil
Methimazole
Thyroid peroxidase inhibitor (oxidation, ionidation, coupling)
PTU or Methimazole in pregnancy?
Ptu=Pregnancy
Methimazole crosses the placental barrier
More potent, PTU or Methimazole?
Methimazole: 10x with longer t1/2
Will destroy fetal thyroid
Peripheral thyronine 5’ deionidase, PTU or Methimazole?
PTU only: tissues cannot convert T4 to T3
AE of PTU?
Rash
Agranulocytosis
What imaging material can kill fetal thyroid?
Radioactive iodine contrast
What two insulin have 1x daily injection?
Insulin glargine
Insulin demetir
How are insulins made to have such a long half life?
isoelectric point increase (with zinc?)
What is the structure of insulin glargine?
B21 asparagine to glycine and 2 asparagines added to Bchain C terminus
What is the pH of insulin demetir?
Acidic solution is neutralized, forming a precipitate
Glucagon
Alpha cells secrete
Opposite of insulin
Elevated in fasting
Used for hypoglycemia rarely, usually just use glucose solution
Glyburide
Sulfonylurea: Block K/ATP channel, causing beta cell depolarization and Ca influx, leading to Insulin release.
DM2
AE: Liver toxicity, hepatitis, hypoglycemia
Repaglinide
Nateglinide
Meglitinides: ATP/K channel, like sulfonylureas.
Benzoic acid derivative.
Taken before meal to control BG after absorption.
AE: Hypoglycemia
Metformin (+glyburide)
Decrease PEPCK and PC in liver, decreasing glucose production.
Stimulate Insulin sensitivity
DM2
AE: lactic acidosis
Fludrocortisone
Aldosterone synthetic
Pioglitazone
Thiazolidinedioines:
PPARy to increase GLUT4 activity
Major drug for increasing insulin sensitivity
What pancreatic tumor is octreotide used for ?
Glucagonoma
Insulinoma
GH release too!
Exanitide
GLP-1 receptor agonist: decrease post prandial glucose
- Make you feel full
- Inhibit glycogen breakdown in liver
- increase insulin secretion for digestion
- Slows gastric emptying
- decrease glucagon secretion
Teriperidide
Pulsatile PTH stimulates bone formation due to PTH–>osteoblasts action without making RANKL.
May stimulate IGF-1.
Important for women post bisphosphonate tx.
Raloxifen
SERM: Selective Estrogen Receptor Modulator
Inhibit osteoclasts
Prevent breast cancer
Osteoporosis approved
Desunomab
RANKL mAb. Blocks osteoclast activtion Prevent bone resorption. Increase bone mass in cancer patients Biannual dose administration
Cincalcinet
Ca Sensing Receptor allosteric binding, allows PTH suppression at lower blood Ca levels.
Lowers PTH.
HyperPTH and PTadenoma Tx
Fluoride
Prevent cavities
Mottles enamel, prevents decay.
Binds to Ca, can prevent clotting.
Toxicity: Osteosclerosis
Cosyntropin: Synthetic ACTH
aa1-24
Prefered to natural due to decreased ADH/AVP content (impurity in animal ACTH)
Cholesevalam
Bile acid sequestrate
Prevent bile (cholesterol) cycling
Semilenthe insulin
Short acting
12 hour insulin
Sitagliptin
Dipeptidyl peptidase 4 inhibitor:
prevents the degradation of incretin (GLP-1) hormones by DP4, allowing GLP-1 to act to increase insulin release
Somatropin
Generic hGH
Menotropin
Menopause FSH/LH purificaiton from urine of old lady used for in vitro ovulatio control
Ganirelix
GnRH receptor antagonist used for in vitro fertilization delay of LH surge and ovulation
