Help
Options
Didn't know it?
click below
click below
Knew it?
click below
click below
Don't Know
Remaining cards (0)
Know
retry
shuffle
restart
0:00
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.
Normal Size Small Size show me how
Normal Size Small Size show me how
IOS 9 Exam 3
Pharmacology of DM drugs
| Question | Answer |
|---|---|
| The major characteristics of exogenous insulin preparations | Degree of purity, concentration, species of origion, time course of action |
| Degree of purity of exogenous insulin | The amount of non-insulin proteins or proinsulin (with C-protein), not a problem anymore (pure<1ppm non-insulin) |
| Concentration of exogenous insulin preparations | Potency of insulin is measured in units. the US standard is 100Units per 1 mL. Highly concentrated insulin is 500Units/1mL |
| Species of origin of exogenous insulin | Is no longer of question since recomninant DNA technology- Proinsulin is inserted in E.coli which produces human proinsulin and C-peptide is cleaved- called human insulin those converted or altered is called analogues |
| Time course of action of exogenous insulin | Onset, peak, duration are the characteristics defining exogenous insulins |
| Rate limiting step of insulin activity is | absorption |
| Absorption of exogenous insulin is affected by (BS- PARC) | Blood flow, site of administration, additives, route of administration, concentration, pH |
| Physiochemical Properties of insulin | Insulin naturally self-associates into hexamers, then dimers , then monomers. Additives such as zinc and protamine stablize the hexamer state |
| Rapid acting insulin analogues are designed to | Mimic physiological post-prandial insulin secretion- Onset-15-30min, peak 1-3 hrs, duration 3-4 hours |
| Short acting insulin analogues PK | Neutral pH buffer w/zinc allows onset 30-60minutes, peak in 2-4hrs, and duration 3-7 hrs |
| Intermediate acting insulin analogues PK | They are neutral protamine hagedorn (phosphate buffer) with onset in 1-2 hrs, peak 6-10hrs, duration-16-20hrs |
| Long acting insulin analogues PK | Glargine contains ph-4 and forms solid depot effect, detemir contains a FA the is highly protein bound- Onset 1-2hrs, Peak-None, Duration 20-24hrs |
| Combination insulins | Humalog mix contains a crystalized lispro (intermediate) and lispro rapid acting others are NPH w/ short acting (regular) |
| Elimination of insulin is via | Kidney via glomular capillaries and degraded by glomerular capillary cells and post glomerular cells |
| Side effects of insulin analogues | Hypoglycemia, wt. gain, lipohypertrophy, lipoatrophy |
| Inhaled insulin PK | Onset is 10-20min, peak 2 hrs, duration 6 hrs...absorption like rapid & duration like short acting |
| Contraindications of inhaled insulin | Smokers (6months), Poorly controlled or unstable lung disease, |
| Side effects of inhaled insulin | Cough, Decline of lung function, Bitter taste |
| Dosing of inhaled insulins | 1mg blister=3units of insulin The 2mg=6units and 3mg=8units |
| Sulfonylurea MOA | Stimulates the B-cells to release insulin ( |
| Sulfonylurea ADME | Abs-90%, Highly protein bound, metabolized via 2C9, renal excretion (hepatic for glipizide) |
| Duration of action for sulfonylureas | Glipizide extended release has special capsule shell that will be found in patients stool |
| Sulfonylurea side effects | Disulfram reaction with 1st generation, tolbutamide and chlorpropamide & ETOH |
| DI of sulfonylureas | Protein binding-(warfarin, sulfa antibiotics, salycilates), Hepatic-(cimetidine, rifampin, MAOs), renal-(allopurinol, probenecid) |
| Short acting secretagologes MOA | Stimulate the B-cells to release insulin at alternative site than Sulfonylureas |
| Short acting secretagologes are | Repaglinide, Nateglinide |
| PK of Short acting secretagologes | Absorption 30-60min, half-life is 1-1.5hr, duration 4 hours |
| Regaglinide metabolism | Via 3A4 hepatic and excreted in the feces |
| Nateglinide metabolism | Via 2C9 and 3A4 hepatic and primary renal excretion |
| DI of Regaglinide | Inducers of 3A4(Grapefruit juice, gemfibrozil, azoles, macrolides, protease inhibtiors) |
| Biguanides MOA | 3- Stope conversion of glycogen to glucose, increase peripheral glucose uptake, decrease GI absor of glucose |
| Metformin ADME | GI absorption, duration of action 12 hr, renal elimination |
| DI of metformin | Cimetidine, trimterene, trimethoprim, digoxin |
| SIde effects of metformin | GI-nausea, diarrhea, metallic taste, weight loss, metabolic acidosis |
| Contraindications of metformin | Scr>1.5 men or >1.4 women, lactic acidosis, liver impairment, CHF +diuretic, Chronic lung disease |
| TZD MOA | Stimulates PPARy which regulates lipid and glucose metabolism or GLUT4 receptor uptake |
| TZD are active on | increasing insulin sensitivity in muscle, liver, and fat. They enhanse glucose utilization and suppress hepatic and lipolysis |
| TZD non-glucose effects | Increase HDL, vascular-decrease inflammation, decrease B-cell decline, move visceral to subcutaneous fat |
| Rosiglitazone is metabolized | by 2C8 and excreted in feces |
| Poiglitazone is metabolized | By 2C8 and 3A4 and excreted in the feces |
| Side effects of TZD | edema, HA, weight gain, anemia |
| DI with TZD's | Rosi=gemfibrizol and Pio-itraconazole |
| Alpha glucosidase inhibitors MOA | Competively inhibit glucosidase in the GI brush boarder to decease glucose absorption |
| PK of alphaglucosidase inhibitors | Acarbose metabolized in GI and excreted in feces, Migitol not metabolized and excreted in urine |
| DI of Alpha glucosidase inhibitors | May decrease digoxin Bioavilability, digestive enzymes, and intestinal adsorbants |
| Pramlintide=Symlin MOA | mimics endogenous amylin decreasing glucagon and delaying gastric emptying, and producing satiety- given SQ prior to meals |
| Side effects of pramlintide | Hypoglycemia (with insulin) , N/V, loss of appetitie, HA |
| Pramlintide DI | May decrease analgesic absorption |
| Byetta MOA | synthetic GLP-1 from Glia monster acts on GLP-1 beta cell to decrease glucagon, increase insulin , sloq gastric emptying, improve satiety |
| Byetta PK | Poor absorption (SQ), eliminated via renal |
| Side effects of byetta | Nausea, weight loss, hypoglycemia (when given with sulfonlyureas) |
| DI of byetta | May decrease absorption of analgesics, and antibiotics |
| Sitagliptin (Januva) MOA | It is a DPP-4 inhibitor thus decreases endogenous breakdown of GLP1 causes decrease in glucagon, increase insulin secretion |
| Sitagliptin ADME | Ok absorption, renal excretion must be dose adjusted CrCl>30 =50mg less than <30=25mg QD |
| SIde effects of sitagliptin | Nausea, diarrhea, slight hypoglycemia |
Created by:
liza001
Popular Pharmacology sets