Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
60 Cards in this Set
- Front
- Back
regular (soluble) insulins for injection
|
bovine (beef)
porcine (pork) ovine (sheep) |
|
modified crystal size insulins
|
- NPH (Neutral, Protamine, Hagedorn or Isophane)
- lente - semilente - ultralente |
|
synthetic insulins: Human Insulins
|
- Humulin (recombinant)
- Novolin (switched aa's from pork) |
|
synthetic insulins: Human Insulin Analogs
|
- Humalog (insulin lispro)
- Novolog (insulin aspart) |
|
synthetic insulins: Shifted Isoelectric Point Insulins
|
- Lantus (insulin glargine)
- Levemir (insulin detemir) |
|
Human Inhaled Insulin Powder
|
Exubera
(not on market anymore) |
|
Oral Hypoglycemics: 1st generation Sulfonylureas
|
Tolbutamide
Chlorpropamide Tolazamide Acetohexamide |
|
Oral Hypoglycemics: 2nd generation Sulfonylureas
|
Glyburide
Glipizide Gliclazide Glimepiride [hint all 2nd gen. sulfonylureas start with "G"] |
|
Oral Hypoglycemics: Meglinitides
|
Repaglinide
Nateglinide |
|
Oral Hypoglycemics: Biguanides
|
- Phenformin (withdrawn, lac. acidosis)
- Metformin - Metformin + glyburide |
|
Oral Hypoglycemics: Thiazolidindiones
|
- Sulfonylureas troglitazone (withdrawn, severe liver tox.)
- Rosiglitazone (black box warning) - Pioglitazone combinations: - Rosiglitazone + metformin - Glipizide + metformin |
|
Oral Hypoglycemics: alpha-Glucosidase Inhibitors
|
Acarbose
Miglitol |
|
Hypoglycemic Drugs: Incretins
(non-oral) |
Exenatide
Sitagliptin |
|
Diazoxide
|
- Anti-hypertensive anti-diuretic with potent hyperglycemic actions
- INHIBITS INSULIN SECRETION (but not synthesis) - txt for various forms of hypoglycemia, such as inoperable insulinomas |
|
Somatostatin
|
- sec. by delta cells of pancreas & also in GI with actions in brain
1. inhibits release of TSH & GH from pituitary 2. inhibits release of insulin & glucagon from pancreas |
|
regular (soluble) insulins for injection
|
bovine (beef)
porcine (pork) ovine (sheep) |
|
modified crystal size insulins
|
- NPH (Neutral, Protamine, Hagedorn or Isophane)
- lente - semilente - ultralente |
|
synthetic insulins: Human Insulins
|
- Humulin (recombinant)
- Novolin (switched aa's from pork) |
|
synthetic insulins: Human Insulin Analogs
|
- Humalog (insulin lispro)
- Novolog (insulin aspart) |
|
synthetic insulins: Shifted Isoelectric Point Insulins
|
- Lantus (insulin glargine)
- Levemir (insulin detemir) |
|
Human Inhaled Insulin Powder
|
Exubera
(not on market anymore) |
|
Oral Hypoglycemics: 1st generation Sulfonylureas
|
Tolbutamide
Chlorpropamide Tolazamide Acetohexamide |
|
Oral Hypoglycemics: 2nd generation Sulfonylureas
|
Glyburide
Glipizide Gliclazide Glimepiride [hint all 2nd gen. sulfonylureas start with "G"] |
|
Oral Hypoglycemics: Meglinitides
|
Repaglinide
Nateglinide |
|
Oral Hypoglycemics: Biguanides
|
- Phenformin (withdrawn, lac. acidosis)
- Metformin - Metformin + glyburide |
|
Oral Hypoglycemics: Thiazolidindiones
|
- Sulfonylureas troglitazone (withdrawn, severe liver tox.)
- Rosiglitazone (black box warning) - Pioglitazone combinations: - Rosiglitazone + metformin - Glipizide + metformin |
|
Oral Hypoglycemics: alpha-Glucosidase Inhibitors
|
Acarbose
Miglitol |
|
Hypoglycemic Drugs: Incretins
(non-oral) |
Exenatide
Sitagliptin |
|
Diazoxide
|
- Anti-hypertensive anti-diuretic with potent hyperglycemic actions
- INHIBITS INSULIN SECRETION (but not synthesis) - txt for various forms of hypoglycemia, such as inoperable insulinomas |
|
Somatostatin
|
- sec. by delta cells of pancreas & also in GI with actions in brain
1. inhibits release of TSH & GH from pituitary 2. inhibits release of insulin & glucagon from pancreas - inhibits insulin in insulomas & inhibits glucagon in glucagomas - short 1/2 life (3-6 min.) |
|
Octreotide
|
- long-acting somatostatin analog
- used for glucagomas -also controls excess secretion of GH (useful in acromegaly) |
|
What are the cellular events leading to Insulin secretion?
|
1. excess blood glucose is taken up by pancreatic B cell (GLUT2) & phosphorylated
2. rise in ATP levels blocks K+ channels, leading to membrane depolarization 3. Influx of CALCIUM causes insulin exocytosis |
|
Stimulants of Insulin Secretion
|
- Glucose, mannose
- Leucine - Vagal stimulation - Sulfonylureas |
|
Amplifiers of Insulin Release
|
Enteric hormones:
- cholecystokinin - secretin - gastrin Neural Stimulation: - beta-adrenergic |
|
Inhibitors of Insulin Release
|
- Somatostatin
- Diazoxide (& other drugs) - Catecholamines |
|
What kind of binding domains does the insulin receptor have?
|
Tyrosine Kinase & ATP binding domains on B subunit
|
|
Proinsulin is converted to Insulin by...?
|
proteolytic cleavage of the C-peptide
(the resultant insulin is composed of A & B chains liked by disulfide bonds) *fun fact: C peptide can serve as an index of insulin secretion |
|
Most important actions of Insulin on LIVER:
|
stimulates conversion of:
1. glucose → glycogen 2. glucose → fatty acids & TAG |
|
Most important actions of Insulin on ADIPOSE TISSUE:
|
stimulates:
1. transport of glucose into cells 2. conversion of glucose to fatty acids & TAG inhibits: release of free fatty acids |
|
Most important actions of Insulin on SKELETAL & CARDIAC MUSCLE:
|
stimulates transport of glucose into cells
|
|
Rapid onset, short duration (short 1/2 life) insulin preparations
|
1. "Regular Insulin"
- crystalline zinc - soluble, clear, only insulin that can be injected IV 2. Semilente |
|
Intermediate onset insulin preparations (slower onset, longer 1/2 life)
|
1. NPH insulin (Neutral, Protamine, Hagedorn or Isophane)
2. LENTE (mixture: 30% semilente/ 70% ultralente zinc insulin crystals) * fun fact: Lente is the most widely used form of insulin |
|
Long acting (longest 1/2 life; largest crystals; slow absorption)
|
Ultralente insulin
|
|
Humulin
|
Human insulin made using recombinant DNA to produce the hormone in bacteria or yeast
|
|
Novolin
|
Human insulin made by switching the amino acid that is different in pork insulin
|
|
Insulin Lispro (Humalog)
|
- analog of Humulin (normal proline B28 & Lysine B29 are switched via modified rDNA)
- doesn't form hexamers (exists in circulation as monomer only) - faster onset of action & shorter 1/2 life than regular insulin |
|
Insulin Aspart (NovoLog)
|
- a rapid acting insulin analog (asp subs. for pro.)
- exists only as a monomer - faster onset of action & shorter 1/2 life |
|
Insulin Glargine (Lantus)
|
- recombinant human insulin analog for use as a injection
- shifted isoelectric point insulin |
|
Insulin Determir
|
- Long-acting (up to 24 hr. duration); this is due to the neutralization of the acidic solution causing crystals to precipitate
- can be injected once a day * low peak insulin concentration decreases chances of NOCTURNAL HYPOGLYCEMIA |
|
Ketoacidosis
|
DIABETIC COMA
cause: low insulin txt: insulin! |
|
Hypoglycemic coma
|
cause: insulin overdose
txt: glucose *very common! |
|
Glycosylated Hemoglobin
|
- test for long-term control of blood glucose
- measures HbA1c results: normal (non-diabetic)~ 6% not good = diab.pt. w/ over 8% dangerous = over 10% [ADA rec. A1C target = 7% or below] |
|
Glucagon
|
- peptide secreted by alpha cells of pancreas
- effects oppose those of insulin - elevated in fasting & diabetes - rarely used for txt.; sometimes in hypoglycemic emergencies but glucose infusion is most often preferred |
|
What do Sulfonylureas do?
|
- increase insulin release (but not after long term txt)
- increase insulin sensitivity by enhancing the effect of insulin on glucose uptake * NSAID's ENHANCE HYPOGLYCEMIC ACTION! |
|
What do Meglitinides do?
|
- increase insulin secretion
- short 1/2 life - taken before each meal to control post-prandial glucose level major SE= hypoglycemia |
|
What do Biguanides do?
|
- decrease hepatic glucose production
- do NOT affect insulin secretion or cause hypoglycemia |
|
What do Thaizolidinediones do?
|
- increase insulin sensitivity
- increase glucose transport into muscles & adipose tissue - bind specifically to PPAR-gamma (Peroxisome Proliferator-Activated Receptor Gamma) |
|
What do alpha-Glucosidase Inhibitors do?
|
- reduce initial absorption of starch, disaccharides by inhibiting brush border alpha-glucosidase
- reduces carb uptake & post-prandial glucose rise - usually used in combination with other hypoglycemic drugs and/or insulin |
|
Exanatide
|
- an Incretin hypoglycemic drug
- improves glycemic control - isolated from Gila monster venom - inhibits glucagon-stimulated glycogenolysis in the liver - May increase production of new beta-calls in the pancreas |
|
Sitagliptin phosphate
|
- an Incretin hypoglycemic drug
- inhibitor of didpeptidyl peptidase-4 (DPP-4), the enzyme that inactivates incretins - inhibits inactivation of GLP-1 |