pharm chart Flashcards
Sulfonylureas 2nd Generation
Glipizide [Glucotrol]
Glipizide [Glucotrol] MOA
Stimulates
pancreatic β-cell
release of insulin
Glipizide [Glucotrol] Indications
T2DM
Meglitinides
Non-Sulfonylurea
Secretagogue
Repaglinide
[Prandin]
MOA of Repaglinide
[Prandin]
binds to sulfonylurea receptor on β-cell to stimulate insulin release
Indications of Repaglinide
[Prandin]
T2DM if sulfa allergy;
↓post-prandial glucose;
↓ A1c 0.6-1.9
↓ Gluc 65-75mg/Dl
Amylin (β-cell)–> released in response to ↑ blood glucose
o Inhibits gastric emptying
o Inhibits glucagon release
Amylin analog
Amylin analog
Pramlintide [Symlin]
MOA of Pramlintide
[Symlin]
Amylin analogue
↓gastric emptying, ↓glucagon secretion, ↓appetite
Indications of Pramlintide
[Symlin]
T1DM, T2DM ↓ postprandial glucose levels
↓ A1c 0.4-0.5
Incretin mimetic: Glucagon-Like Peptide-1 Agonist (GLP-1)
Synthetic analogue
What are the two drugs?
Exenatide [Byetta]
Liraglutide [Victoza]
MOA of Exenatide
[Byetta]
↑insulin release;
↓glucagon release;
↓gastric emptying;
↓appetite
Indications of Exenatide
[Byetta]
T2DM w/ metformin,
+/- sulfonylurea to lower postprandial glucose levels
↓ A1c 0.5 - 1.0%
MOA of Liraglutide
[Victoza]
↑insulin release; ↓glucagon release; ↓gastric emptying; ↓appetite ↑ β-cell growth/replication
Indications of Liraglutide
[Victoza]
T2DM w/ metformin,
+/- sulfonylurea to
lower postprandial glucose levels
Dipeptidyl peptidase-4 inhibitors
DPP-4 Inhibitors
Sitagliptin
[Januvia]
MOA of Sitagliptin
[Januvia]
Inhibits DPP-4 to reduce degradation of GLP-1 –> incr levels of GLP-1; reduces postprandial glucose levels
Indications of Sitagliptin
[Januvia]
T2DM
Rapid Acting Insulin
Lispro
[Humalog]
MOA of Lispro
[Humalog]
insulin replacement,
supplement
Indications of Lispro
[Humalog]
T1DM
T2DM
Short-Acting
Insulin
Regular
[Humulin-R]
MOA of Regular
[Humulin-R]
insulin replacement,
supplement
Indications of Regular
[Humulin-R]
T1DM
T2DM
Intermediate- Acting Insulin
Neutral
Protamine
[Humulin-N]
MOA of Neutral Protamine
[Humulin-N]
insulin replacement,
supplement
Indications of Neutral Protamine
[Humulin-N]
T1DM,
T2DM
Long-Acting Insulin
100u/mL
Insulin Glargine
[Lantus]
MOA of Insulin Glargine
[Lantus]
insulin replacement,
supplement
Indications of Insulin Glargine
[Lantus]
T1DM,
T2DM
Long-Acting Insulin
300u/mL
Insulin Glargine
[Toujeo Solostar]
MOA Insulin Glargine
[Toujeo Solostar]
insulin replacement,
supplement
Indications of Insulin Glargine
[Toujeo Solostar]
T1DM,
T2DM
Oral Inhalation, Rapid Acting Insulin
Human rDNA Insulin
[Afrezza]
MOA of Human rDNA Insulin
[Afrezza]
Inhaled insulin
Indications of Human rDNA Insulin
[Afrezza]
T1DM,
T2DM
used w/longacting
insulin
Biguanides
Metformin
[Glucophage]
MOA of Metformin
[Glucophage]
unknown mechanism to decr hepatic glucose production, decr renal gluconeogenesis, slow intestinal absorption glucose, incr glucose conversion to lactate by enterocytes, stim tissue glycolysis, incr glucose removal from blood (decr insulin resistance), decr plasma glucagon levels
Indications of Metformin
[Glucophage]
T2DM
Initial DOC
Thiazolidinediones
TZD’s
Pioglitizone
[Actos]
MOA of Pioglitizone
[Actos]
decr insulin resistance
by activation of nuclear PPAR-ϒ in myocytes, hepatocytes, adipocytes;
most potent insulin sensitizer;
pioglit also PPAR-α activity (incr trig metab)
Indications of Pioglitizone
[Actos]
T2DM
α-glucosidase
Inhibitors
Acarbose
[Precose]
MOA of Acarbose
[Precose]
reduces postprandial glucose levels by inhibition intestinal α-glucosidase conversion polysaccrides to monoscaccrides;
delays absorption & levels blood glucose
Indications of Acarbose
[Precose]
T1DM,
T2DM
SGLT2 Inhibitor Sodium-Glucose
CoTransportor 2
Canaglifloxin
[Invokana]
MOA of Canaglifloxin
[Invokana]
inhibits glucose resorption in proximal renal tubule
Indications of Canaglifloxin
[Invokana]
Adjunct therapy in T2DM
Not T1DM
Bile Acid Sequestrant
Colesevelam
[Welchol]
MOA of Colesevelam
[Welchol]
unknown in DM
(decrease intestinal
glucose absorption?)
Indications Colesevelam
[Welchol]
hypercholest erolemia;
adjunct to metformin,
sulfonylurea, insulin in T2DM
Vasopressin Receptor Agonists
Desmopressin
[DDAVP]
MOA of Desmopressin
[DDAVP]
incr permeability of renal tubular cells to water
resorption→ decr urine volume;
incr vonW factor, VIII, t-PA levels
Indication Desmopressin
[DDAVP]
diabetes insipidus;
primary nocturnal enuresis;
(off label) to control uremic bleeding; bleeding in hemophilia
Adjunct Drugs:
ACEI / ARBs
HMGCoARI (‘statins’)
ASA
Estrogens
Conjugated
estrogens
Selective Estrogen
Receptor
Modulators
(SERMs)
Raloxifine
[Evista
MOA of Raloxifine
[Evista
binds to selected estrogen
recepters and decr bone
resorption
Indications of Raloxifine
[Evista
Px & Tx
osteoporosis
Bisphosphenate:
Oral
Alendronate
[Fosamax]
MOA of Alendronate
[Fosamax]
decreases rate bone
resorption
indication Alendronate
[Fosamax]
Px & Tx of osteoporosis
in women; Tx in men;
Paget’s Disease
Bisphosphenate:
IV
Zoledronic Acid
[Reclast]
MOA of Zoledronic Acid
[Reclast]
Inhibits osteoclast activity
and skeletal calcium
release
Indications of Zoledronic Acid
[Reclast]
Px & Tx Osteoporosis; Tx multiple myeloma, metastatic bone lesions; hypercalcemia of malignancy, Paget’s Disease
RANK Ligand Inhibitor
Denosumab
[Prolia]
MOA of Denosumab
[Prolia]
Human monoclonal antibody which attaches to RANKL blocking
ability to bind to RANK receptor on surface of osteoclast thereby
inhibiting osteoclastogenesis &
increasing osteoclast apoptosis
Indications of Denosumab
[Prolia]
Males and postmenopausal females at high fracture risk d/t osteoporosis; men on androgen deprivation rx and women
receiving aromatase inhibitor rx
Calcitonin Hormone
Calcitonin Salmon
[Miacalcin]
MOa of Calcitonin
Salmon
[Miacalcin]
protein sequence similar to human calcitonin; antagoizes impact of parathyroid hormone & inhibits osteoclast activity
Indications of Calcitonin
Salmon
[Miacalcin]
osteoporosis,
Paget’s
disease,
hypercalcemia
Recombinant Human Parathyroid
Hormone
Fragment Hormone
Teriparatide
[Forteo]
MOA of Teriparatide
[Forteo]
recombinant form PTH (1-34);
stim new bone formation
Indications of Teriparatide
[Forteo]
Tx severe,
treatment resistant osteoporosis
(max 2 years use)
Thyroid Agents
synthetic T4 replacement
Levothyroxine (T4)
[Levothroid, Levoxyl, Synthroid]
MOA of Levothyroxine (T4)
[Levothroid, Levoxyl, Synthroid]
replacement T4
converted to T3 in peripheral tissues–> nuclear receptors–>
protein synthesis, metabolic rate,
promotes gluconeogeesis
Indications of Levothyroxine (T4)
[Levothroid, Levoxyl, Synthroid]
Hypothyroidism
Thyroid CA
Thyroid Agents
synthetic T3 replacement
Liothyronine (T3)
[Cytomel]
MOA of Liothyronine (T3)
[Cytomel]
T3 in peripheral tissues --> nuclear receptors --> protein synthesis, metabolic rate, promotes gluconeogenesis
Indications of Liothyronine (T3)
[Cytomel]
hypothyroidism not responsive to T4 Tx Tx of myxedema coma
Thyroid
Ablation
Radioactive
iodine (131 I) RAI
MOA of Radioactive
iodine (131 I) RAI
radioactive iodine is concentrated in thyroid gland w/ death of gland cells over 6-8wks
Indications of Radioactive
iodine (131 I) RAI
thyroid ablation
w/o surgery
Antithyroid Agents
Methimazole
[Tapazole]
MOA of Methimazole
[Tapazole]
Blocks oxidation of iodine in thyroid gland preventing iodine combining w/ tyrosine to form T4, T3 doesn't inactivate circulating T4, T3
Indications of Methimazole
[Tapazole]
hyperthyroidism
Antithyroid Agents
Thiamine
Propylthiouracil
[PTU}
MOA of Propylthiouracil
[PTU}
interfere w/ thyroid hormone synthesis; inhibits conversion T4 to T3; has immunosuppressive effects (bone marrow)
Indications of Propylthiouracil
[PTU}
Graves disease, pre-thyroid surgery or RAI131 therapy; thyrotoxic crisis
Glucocorticoid
Intermediate acting
(T1/2= 12-36H)
2 drugs
- Prednisone
2. Prednisolone [Omnipred]
MOA of Glucocorticoid
Intermediate acting
suppresses adrenal function at high dose; decreased leukocyte migration; enters cell nucleus to alters synthesis of proteins
Indications of Glucocorticoid
Intermediate acting
multiple
immunosuppress
ive fxns
what is important to remember about Prednisolone [Omnipred]
Same as Prednisone
Active form of prednisone
Glucocorticoid Long acting
T1/2 >48H
Dexamethasone
[Maxidex]
what to know about Dexamethasone
[Maxidex]
Same as Prednisone
Much more potent than predniseon (~7-10x)
Equiv dosing —> prednisone 5mg = dexamethasone 0.75mg
Mineralcorticoid
Fludrocortisone
[Florinef]
MOA of Fludrocortisone
[Florinef]
promotes increase distal
renal tubule absorp
of Na+ & loss of K+
Indications of Fludrocortisone
[Florinef]
Addisons ds (adrenocotical insufficiency) resistant orothostatic hypotension
Adjunct Drugs:
Beta Blockers
Propanolol
Metoprolol