Class: Biguanides MOA: 1. )Decreases hepatic glucose production mainly by inhibiting gluconeogenesis via inhibition of enzyme activities. Reduces hepatic uptake of gluconeogenic substrates (lactate included!) 2. ) Increases insulin sensitivity, reducing lipolysis and glucose absorbtion from the intestine. Via suppression of respiratory chain. Increased insulin TK activity. Stimulation of GLUT4. Side effects: Diarrhea w/ high intial dose. Lactic Acidosis Oral No hypoglycemia; Weight neutral (loss)

Rapid acting insulin Onset: 15 min. Max: 0.5-1.5hr. Duration: 3-4hrs. no LAG insulin (Lispro, Aspart, Glulisine) Side effects: 1. )Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.) 2. ) Weight gain (loss of leaking calories) 3. ) Allergic reactions/ Skin probs/ Insulin resistance

Short acting insulin Onset: 30 min Max: 2-3hrs. Duration: 4-8hrs. Side effects: 1. )Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.) 2. ) Weight gain (loss of leaking calories) 3. ) Allergic reactions/ Skin probs/ Insulin resistance

Drugs Test 1 Flashcards by Mike Rose

Metformin

Class: Biguanides

MOA:

)Decreases hepatic glucose production mainly by inhibiting gluconeogenesis via inhibition of enzyme activities. Reduces hepatic uptake of gluconeogenic substrates (lactate included!)
) Increases insulin sensitivity, reducing lipolysis and glucose absorbtion from the intestine. Via suppression of respiratory chain. Increased insulin TK activity. Stimulation of GLUT4.

Side effects: Diarrhea w/ high intial dose. Lactic Acidosis

Oral

No hypoglycemia; Weight neutral (loss)

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Glimiperide

Class: Sulfonylureas (2nd Gen)

MOA: Insulin secretagogue. Binds SUR1 subunit of the K+ATP channel –> closes –> Ca++ entry and depol –> increased insulin release.

Must have some Beta-cell function to be effective

Oral

Side effects: Hypoglycemia and weight gain.

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Exanitide

Class: Incretins

MOA: Glucagon-like Peptide 1 (GLP-1) analog. Increases cAMP levels in beta-cells –> stimulates insulin secretion and inhibitis glucagon secretion. Delays gastric emptying –> promotes satiety.

SubQ before meal

Side effect: Pancreatitis; GI problems

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Sitagliptin

Class: Dipetidyl peptidase IV inhibitors

MOA: Inhibits DDP-IV which increases incretin activity (inhibits glucagon and stimulates insulin release). Delays gastric emptying –> satiety

Oral

Not associated w/ hypoglycemia and weight gain.

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Repaglinide

Class: Meglitinides

MOA: Insulin secretagogues. K+ channel blocker.

Oral, take w/ meal

Hypoglycemia and weight gain.

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Nataglinide

Class: Meglitinides

MOA: Insulin secretagogues. K+ channel blocker.

Oral, take w/ meal

Hypoglycemia and weight gain.

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Acarbose

Class: Alpha glucosidase inhibitor

MOA: Inhibit hydrolysis of disaccharides and complex carbs to monosaccharides. Lowers postprandial glucose levels.

Side effects: GI

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Miglitol

Class: Alpha glucosidase inhibitor

MOA: Inhibit hydrolysis of disaccharides and complex carbs to monosaccharides. Lowers postprandial glucose levels.

Side effects: GI

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Pramlinitide

Class: Amylin Analog

MOA: Binds amylin receptors to inhibit glucagon. Delays gastric emptying.

SubQ

Can cause severe hypoglycemia in combination w/ insulin.

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Rosaglitazone

Class: Thiozolidenes

MOA: PPARgamma (+/-) PPARalpha receptor agonists. Belong to steroid receptor family and affect transcription. Increase glucose uptake and utilization by increasing GLUT transporters.

Requires insulin to be present.

Oral

Side effects: Weight gain, Heart failure, URI, Hepatoxic

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Piaglitazone

Class: Thiozolidenes

MOA: PPARgamma (+/-) PPARalpha receptor agonists. Belong to steroid receptor family and affect transcription. Increase glucose uptake and utilization by increasing GLUT transporters.

Requires insulin to be present.

Oral

Side effects: Weight gain, Heart failure, URI, Hepatoxic, and increased bladder cancer risk.

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Glyburide

Class: Sulfonylureas (2nd Gen)

MOA: Insulin secretagogue. Binds SUR1 subunit of the K+ATP channel –> closes –> Ca++ entry and depol –> increased insulin release.

Must have some Beta-cell function to be effective

Oral

Side effects: Hypoglycemia and weight gain.

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Glipizide

Class: Sulfonylureas (2nd Gen)

MOA: Insulin secretagogue. Binds SUR1 subunit of the K+ATP channel –> closes –> Ca++ entry and depol –> increased insulin release.

Must have some Beta-cell function to be effective

Oral

Side effects: Hypoglycemia and weight gain.

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Chlorpromide

Class: Sulfonylureas (1st Gen)

MOA: Insulin secretagogue. Binds SUR1 subunit of the K+ATP channel –> closes –> Ca++ entry and depol –> increased insulin release.

Must have some Beta-cell function to be effective

Oral

Side effects: Hypoglycemia and weight gain. Disulfiram.

Not used anymore –> side effects (due to long half life) and less potent

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Lispro

Rapid acting insulin

Onset: 15 min.

Max: 0.5-1.5hr.

Duration: 3-4hrs.

no LAG insulin (Lispro, Aspart, Glulisine)

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

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Aspart

Rapid acting insulin

Onset: 15 min.

Max: 0.5-1.5hr.

Duration: 3-4hrs.

no LAG insulin (Lispro, Aspart, Glulisine)

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

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Glulisine

Rapid acting insulin

Onset: 15 min.

Max: 0.5-1.5hr.

Duration: 3-4hrs.

no LAG insulin (Lispro, Aspart, Glulisine)

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

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Regular insulin

Short acting insulin

Onset: 30 min

Max: 2-3hrs.

Duration: 4-8hrs.

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

NPH Insulin

Intermediate acting insulin

Onset: 2-4hrs

Max: 4-12 hrs.

Duration: 10-20 hrs.

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

Glargine

Long Acting Insulin

Onset: 1-2 hrs.

Max: no peak

Duration 18-24hrs.

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

Detemir Insulin

Long acting insulin

Onset: 1-2

Max: no peak

Duration 18-24

Side effects:

)Hypoglycemia (sweating, hunger, anxiety, tremor, palpitations are early. Difficulty concentrating, weakness, drowsiness, dizziness, blurred vision, loss of consciousness are late.)
) Weight gain (loss of leaking calories)
) Allergic reactions/ Skin probs/ Insulin resistance

Cortisol

Glucorticoid: 1

Mineralocorticoid: 1

Prednisone

Glucorticoid: 3.5-5

Mineralocorticoid: 0.8

Methylprednisilone

Glucocorticoid: 5-7.5

Mineralocorticoid: 0.5

Dexamethasone

Glucocorticoid: 25-80 Mineralocorticoid: 0

Fludrocortisone

Glucocorticoid: 15 Mineralocorticoid: 200 Used as aldosterone replacement

Prednisilone

Glucocorticoid: 4 Mineralocorticoid: 0.8

Betamethasone

Glucocorticoid: 25-30 Mineralocorticoid: 0

Triamcinolone

Glucocorticoid: 5 Mineralocorticoid: 0

Deoxycorticosterone acetate (DOCA)

Glucocorticoid: 0 Mineralocorticoid: 20

Aldosterone

Glucocorticoid: 0.3 Mineralocorticoid: 200-1000

ACTH

Distinguishes from primary and secondary adrenal insufficiency. Anticonvulsant for infantile spasms and to prevent neurotoxicity w/ cisplatin.

Ketoconazole

MOA: Inhibits side change cleavage and other CYP enzymes --> decreased steroid synthesis. Blocks glucorticoid and androgen synthesis. Side effects: Hepatotoxic

Metyrapone

Inhibits 11 beta hydroxylase in the adrenal gland with the goal of interfering with cortisol production. May be used when waiting for a definitive dx

Cabergoline

Dopamine agonist that can be used to treat pituitary adenomas.

Mifepristone

Glucocorticoid receptor antagonist. Used for patients w/ inoperable ACTH secreting tumors.

Mitotane

DDT class of insecticides w/ nonselective adrenal toxicity.

Sermorelin

GHRH analog. Can be used w/ arginine in co-stimulation test to find source of GH deficiency.

Somatotropin

Recombinant human growth hormone GH can be used to treat hyposecretion syndromes in children Hypopituitarism (most commonly hormone def. is GH; 1/4000 births). Idiopathic short stature Turner syndrome growth deficiency SHOX mutations Trauma that disrupts GH release. Goal is to give GH to maintain IGF-1 in normal range Side effects: scoliosis, diabetogenic Also used in muscle wasting syndrome associated w/ AIDS Potential for abuse by body-builders Laron-type won't be reactive (mutated receptor)

Mecasermine

Recombinant IGF-1 Stimulates growth. Not as effective as GH in kids who respond to GH. Fewer negative side effects. Side effects: hypoglycemia (give before a meal). Don't give to kids w/ cancer (growth promoter!). Don't give if epiphyseal plates are closed.

Bromocriptine

Dopamine (D2) agonist which act on Gi--> decreasing cAMP. Used to treat pituitary adenoma secreting GH or in lack of prolactin.

Cabergoline

Dopamine (D2) agonist which act on Gi--> decreasing cAMP. Used to treat pituitary adenoma secreting GH or in lack of prolactin. Preferred rx for prolactinoma

Octreotide

Long acitng somatostatin analog that works via Gi. Used in GH secreting pituitary adenoma. Side effects: loos stools, cramps, malabsorbtion, etc. Also used in: Carcinoid syndrome, esophageal varices, gastric dumping syndrome, VIPoma, gastrinoma

Pegvisomant

GH antagonist that block hepatic GH receptors --> prevent IGF-1 release. Reduced IGF-1 may increase GH by negative feedback. Side effects: Hepatoxicity

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Drugs Test 1 Flashcards

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