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60 Cards in this Set
- Front
- Back
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regular (soluble) insulins for injection
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bovine (beef)
porcine (pork) ovine (sheep) |
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modified crystal size insulins
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- NPH (Neutral, Protamine, Hagedorn or Isophane)
- lente - semilente - ultralente |
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synthetic insulins: Human Insulins
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- Humulin (recombinant)
- Novolin (switched aa's from pork) |
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synthetic insulins: Human Insulin Analogs
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- Humalog (insulin lispro)
- Novolog (insulin aspart) |
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synthetic insulins: Shifted Isoelectric Point Insulins
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- Lantus (insulin glargine)
- Levemir (insulin detemir) |
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Human Inhaled Insulin Powder
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Exubera
(not on market anymore) |
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Oral Hypoglycemics: 1st generation Sulfonylureas
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Tolbutamide
Chlorpropamide Tolazamide Acetohexamide |
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Oral Hypoglycemics: 2nd generation Sulfonylureas
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Glyburide
Glipizide Gliclazide Glimepiride [hint all 2nd gen. sulfonylureas start with "G"] |
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Oral Hypoglycemics: Meglinitides
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Repaglinide
Nateglinide |
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Oral Hypoglycemics: Biguanides
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- Phenformin (withdrawn, lac. acidosis)
- Metformin - Metformin + glyburide |
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Oral Hypoglycemics: Thiazolidindiones
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- Sulfonylureas troglitazone (withdrawn, severe liver tox.)
- Rosiglitazone (black box warning) - Pioglitazone combinations: - Rosiglitazone + metformin - Glipizide + metformin |
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Oral Hypoglycemics: alpha-Glucosidase Inhibitors
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Acarbose
Miglitol |
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Hypoglycemic Drugs: Incretins
(non-oral) |
Exenatide
Sitagliptin |
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Diazoxide
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- Anti-hypertensive anti-diuretic with potent hyperglycemic actions
- INHIBITS INSULIN SECRETION (but not synthesis) - txt for various forms of hypoglycemia, such as inoperable insulinomas |
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Somatostatin
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- 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 |
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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"] |
|
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Oral Hypoglycemics: Meglinitides
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Repaglinide
Nateglinide |
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Oral Hypoglycemics: Biguanides
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- Phenformin (withdrawn, lac. acidosis)
- Metformin - Metformin + glyburide |
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Oral Hypoglycemics: Thiazolidindiones
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- Sulfonylureas troglitazone (withdrawn, severe liver tox.)
- Rosiglitazone (black box warning) - Pioglitazone combinations: - Rosiglitazone + metformin - Glipizide + metformin |
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Oral Hypoglycemics: alpha-Glucosidase Inhibitors
|
Acarbose
Miglitol |
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|
Hypoglycemic Drugs: Incretins
(non-oral) |
Exenatide
Sitagliptin |
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Diazoxide
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- Anti-hypertensive anti-diuretic with potent hyperglycemic actions
- INHIBITS INSULIN SECRETION (but not synthesis) - txt for various forms of hypoglycemia, such as inoperable insulinomas |
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Somatostatin
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- 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.) |
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Octreotide
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- long-acting somatostatin analog
- used for glucagomas -also controls excess secretion of GH (useful in acromegaly) |
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What are the cellular events leading to Insulin secretion?
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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 |
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Stimulants of Insulin Secretion
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- Glucose, mannose
- Leucine - Vagal stimulation - Sulfonylureas |
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Amplifiers of Insulin Release
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Enteric hormones:
- cholecystokinin - secretin - gastrin Neural Stimulation: - beta-adrenergic |
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Inhibitors of Insulin Release
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- Somatostatin
- Diazoxide (& other drugs) - Catecholamines |
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What kind of binding domains does the insulin receptor have?
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Tyrosine Kinase & ATP binding domains on B subunit
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Proinsulin is converted to Insulin by...?
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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 |
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Most important actions of Insulin on LIVER:
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stimulates conversion of:
1. glucose → glycogen 2. glucose → fatty acids & TAG |
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Most important actions of Insulin on ADIPOSE TISSUE:
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stimulates:
1. transport of glucose into cells 2. conversion of glucose to fatty acids & TAG inhibits: release of free fatty acids |
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Most important actions of Insulin on SKELETAL & CARDIAC MUSCLE:
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stimulates transport of glucose into cells
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Rapid onset, short duration (short 1/2 life) insulin preparations
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1. "Regular Insulin"
- crystalline zinc - soluble, clear, only insulin that can be injected IV 2. Semilente |
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Intermediate onset insulin preparations (slower onset, longer 1/2 life)
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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 |
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Long acting (longest 1/2 life; largest crystals; slow absorption)
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Ultralente insulin
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Humulin
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Human insulin made using recombinant DNA to produce the hormone in bacteria or yeast
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Novolin
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Human insulin made by switching the amino acid that is different in pork insulin
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Insulin Lispro (Humalog)
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- 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 |
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Insulin Aspart (NovoLog)
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- a rapid acting insulin analog (asp subs. for pro.)
- exists only as a monomer - faster onset of action & shorter 1/2 life |
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Insulin Glargine (Lantus)
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- recombinant human insulin analog for use as a injection
- shifted isoelectric point insulin |
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Insulin Determir
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- 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 |
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Ketoacidosis
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DIABETIC COMA
cause: low insulin txt: insulin! |
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Hypoglycemic coma
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cause: insulin overdose
txt: glucose *very common! |
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Glycosylated Hemoglobin
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- 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] |
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Glucagon
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- 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 |
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What do Sulfonylureas do?
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- 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! |
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What do Meglitinides do?
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- increase insulin secretion
- short 1/2 life - taken before each meal to control post-prandial glucose level major SE= hypoglycemia |
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What do Biguanides do?
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- decrease hepatic glucose production
- do NOT affect insulin secretion or cause hypoglycemia |
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What do Thaizolidinediones do?
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- increase insulin sensitivity
- increase glucose transport into muscles & adipose tissue - bind specifically to PPAR-gamma (Peroxisome Proliferator-Activated Receptor Gamma) |
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What do alpha-Glucosidase Inhibitors do?
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- 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 |
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Exanatide
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- 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 |
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Sitagliptin phosphate
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- an Incretin hypoglycemic drug
- inhibitor of didpeptidyl peptidase-4 (DPP-4), the enzyme that inactivates incretins - inhibits inactivation of GLP-1 |
