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Endo Exam 2 MED CHEM
| Question | Answer |
|---|---|
| WHAT SECRETES INSULIN | BETA CELLS OF ISLET OF LANGERHANS |
| SHORT ACTING INSULIN | HUMILIN R, NOVOLIN R |
| SHORT ACTING INSULIN ONSET OF ACTION AND DURATION | OA: 0.5-1 HR DOA: 6-8 HR |
| RAPID ACTING INSULIN | LISPRO (HUMALOG) ASPART (NOVOLOG) GLULISINE (APIDRA) |
| RAPID ACTING INSULIN ONSET OF ACTION AND DURATION | OA: 15 MIN DOA: 4 HR |
| LISPRO (HUMALOG) SEQUENCE CHANGES (2) | B28 PRO -> LYS B29 LYS -> PRO |
| ASPART( NOVOLOG) SEQUENCE CHANGE | B28 PRO -> ASP |
| GLULISINE (APIDRA) SEQUENCE CHANGES (2) | B3 ASN -> LYS B29 LYS -> GLU |
| WHAT MAKES RAPID INSULIN HAVE A FAST DURATION OF ACTION? | EXIST AS MONOMERS |
| WHATS THE NAME OF THE INHALED INSULIN? DURATION? CONTRAINDICATION? | -AFREZZA -90-270 MIN - CHRONIC LUNG DISEASE/ BRONCHO SPASMS |
| INTERMEDIATE-ACTING INSULIN | HUMULIN N NOVOLIN N |
| INTERMEDIATE ACTING INSULIN IS COMPLEXED WITH WHAT ? (2) | PROTAMINE (POSITIVELY CHARGED) AND REGULAR INSULIN (HUMILIN AND NOVOLIN R) |
| WHAT IS THE INTERMEDIATE ACTING INSULIN APPEARANCE? ONSET OF ACTION? DURATION? | CLOUDY OA: 2 HR DOA; 12-18 HR |
| LONG ACTING INSULIN | GLARGINE (LANTUS) DETEMIR ( LEVEMIR) DEGLUDEC (TRESIBA) |
| WHAT SEQUENCE CHANGES OCCUR IN GLARGINE (LANTUS)? | GLYSINE & ARGININE |
| WHAT MAKES GLARGINE LONG ACTING ? | PH4 IN SOLUTION BUT WHEN INJECTED AT BODY PH IT PRECIPITATES AND TAKES LONGER TO BE RELEASED |
| GLARGINE ONSET AND DOA | OA: 2 HR DOA;20-24 HR |
| WHAT SEQUENCE CHANGE OCCURS IN DETEMIR ? | ADD C14 FATTY ACID (MYRISTIC ACID) TO B 29 LYS AND BINDS TO ALBUMIN AND LONGER ACTION |
| DETEMIR ONSET AND DOA? | OA: 2HR DOA : 12-24 |
| WHAT SEQUENCE OCCURS TO DEGLUDEC ? | REMOVAL OF THREONINE AND ADD GLUTAMIC ACID AND HEXADECANEDIOIC FATTY ACID |
| DEGLUDEC OA & DOA | OA: 1 HR DOA: > 24 HRS ULTRA LONG INSULIN |
| WHAT MEDICATIONS CAN CAUSE HYPERGLYCEMIA? (5) | -GLUCOCORTICOIDS -NIACIN -DIURETICS (THIAZIDES) -HYDANTOINS (PHENYTOIN) -ATYPICAL ANTIPSYCHOTICS |
| WHAT MEDICATIONS CAN CAUSE HYPOGLYCEMIA? (3) | -PO DIABETIC MEDS -ACEi -SALICYLATES |
| WHAT IS INSULIN? | PEPTIDE |
| IS GLP-1 A DRUG BY ITSELF? WHAT SECRETES INCRETIN? | NO INTESTINAL L-CELLS |
| WHAT HYDROLYZES GLP-1? | DPP-IV (DIPEPIDYLPROTEASE) |
| WHAT EFFECT DOES GLP-1 HAVE ON INSULIN AND GLUCAGON AND FOOD INTAKE, BLOOD GLUCOSE | -INCREASES INSULIN SECRETION -DECREASES GLUCAGON RELEASE -DECREASE FOOD INTAKE -DELAYS GASTRIC EMPTYING -DECREASES BLOOD GLUCOSE |
| HOW MANY AA PEPTIDES DOES GLP-1 HAVE? | 37 INCRETIN HORMONES |
| WHERE DOES THE ENZYME DPP-IV CLEAVE TO HYDROLYZE GLP-1? | BETWEEN 8 ALA & 9 GLU |
| GLP-1 BBW? | RISK OF THYROID TUMORS |
| WHAT IS THE EXENATIDE HOMOLOGY PERCENTAGE | 53% |
| EXENATIDE ER (BYDUREON) LASTS 2 WEEKS BECAUSE ITS FORMULATED AS? | MICROSPHERES |
| WHAT MAKES LIRAGLUTIDE NOT HYDRALYZABLE BY DPP-IV AND LASTS 13 HOURS? | ADDITION OF C16 FATTY ACID CHAIN ATTACH TO 2 LYS |
| WHAT MAKES DULAGLUTIDE NOT HYDRALYZABLE BY DPP-IV AND LASTS 5 DAYS? HOW OFTEN IS IT ADMINISTERED? | -GLP-1 ANALOG + LINKER + MODIFIED IgG4 FC DOMAIN -ONCE A WEEK |
| (1) WHAT AA SEQUENCE CHANGE OCCURS IN SEMAGLUTIDE? | AA 8 ALANINE CHANGES TO ALPHA-AMINOISOBUTYRIC ACID BY STERIC HINDRANCE AND CANT BE HYDROLYZED BY DPP-IV |
| (2) WHAT AA SEQUENCE CHANGE OCCURS IN SEMAGLUTIDE? | AA 26 LYS ATTATCHED TO SPACER AND CONTAINS C-18 FATTY DI-ACID CHAIN |
| HOW IS SEMAGLUTIDE ORAL FORMULATED? | -WHEN SEMAGLUTIDE GETS TO THE STOMACH IT STARTS TO DISSOLVE AND RELEASES SNAC. SNAC RAISES LOCAL PH AND PREVENTS DEGRADATION OF SEMAGLUTIDE. |
| WHAT CLASS DOES TIRZEPATIDE BELONG TO ? HOW OFTEN IS IT ADMINISTERED? | GLP-1 AGONIST AND GIP ONCE A WEEK |
| WHAT RELEASES PRAMLINTIDE ? WHAT IS COSECRETED WITH PRAMLINTIDE? | -BETA CELLS -INSULIN |
| IS PRAMLINTIDE SUITABLE AS A DRUG? | NO |
| WHAT ROLES DO AMYLIN AGONIST PLAY? | - SUPPRESS GLUCAGON SECRETION -REGULATE FOOD INTAKE |
| SUBSTITUTION WITH PROLINE IN PRAMLINTIDE HAS WHAT EFFECT ON WATER SOLUBILITY AND SELF-AGGREGATION? | -INCREASE -DECREASE |
| WHERE DO SULFONYLUREAS BIND TO? WHAT DO THEY STIMULATE TO RELEASE? | -SUR OF THE ATP-SENSITIVE K CHANNELL ON BETA CELLS -INSULIN |
| WHERE ELSE DO SULFONYLUREAS BIND THAT THEY CAUSE SIDE EFFECTS SUCH AS CARDIAC EFFECTS? | -CARDIAC AND SMOOTH MUSCLES |
| SECOND GEN SULFONYLUREAS ARE MORE BULKY, POTENT AND CONTAIN CYCLIC ALIPHATIC GROUPS TRUE OR FALSE? | TRUE |
| SULFONAMIDES ARE HIGHLY PROTEIN BOUND, WHAT HAPPENS WHEN YOU COMBINE DRUGS SUCH AS WARFARIN, SALICYLATES WITH SULFONYLUREAS? | THEY WILL DISPLACE SULFONYLUREAS AND CREATE MORE FREE FORM DRUG AND RESULT IN HYPOGLYCEMIA |
| WHAT 2 DRUGS ARE MEGLITINIDES? | -REPAGLINIDE -NATEGLINIDE |
| WHAT IS THE DOA FOR SULFONYLUREAS | ABOUT 24 HOURS |
| WHAT IS THE DOA FOR MEGLITINIDES? | 4-6 HOURS |
| MEGLITINIDES CAN CUASE HYPOGLYCEMIA TRUE OR FALSE? | TRUE, BUT FOR A SHORTER PERIOD OF TIME |
| WHERE DOES NATEGLINIDE BINDS SELECTIVELY AT? MORE OR LESS CV SIDE EFFECTS? | -SUR1 ON BETA CELLS OF PANCREAS -LESS SIDE EFFECTS |
| HOW IS METFORMIN TRANSPORTED? | ORGANIC CATION TRANSPORTER (OCT) |
| METFORMIN SERIOUS BUT RARE SE? -WHO HAS HIGHER RISK? | -LACTIC ACIDOSIS - RENAL OR HEPATIC IMPAIREMENT, ALCOHOL ABUSE, CHF |
| METFORMIN DDI WITH THIS DRUG DUE TO BOTH USING OCT? (INCREASES METFORMIN CONCENTRATION) | CIMETIDINE (ANTIHISTAMINE) |
| METFORMIN IS CI WITH ? | IODINATED CONTRAST AGENTS |
| MOA OF THIAZOLIDINEDIONES (TZD) PIOGLITAZONES | PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR-Y) STIMULATION |
| ACTOS HAS DDI WITH WHICH CYPS? | -2C8 INHIBITOR GEMFIBROZIL -2C8 INDUCER RIFAMPIN |
| ACTOS SE ? | -CHF -WEIGHT GAIN -EDEMA -BONE FRACTURES IN FEMALES |
| DPP-IV INHIBITORS END IN ? | GLIPTIN |
| INCRETIN HORMONES (2) | -GLP-1 -GIP |
| SITAGLIPTIN | JANUVIA |
| SAXAGLIPTIN CONTAINS WHAT GROUP TO INCREASE LIPOPHILICITY? WHAT BOND DOES IT FORM WITH SER 630? BRAND NAME? | -ADAMANTYL (HAT) -COVALENT IRREVERSIBLE -ONGLYZA |
| LINAGLIPTIN BRAND NAME DOES IT NEED TO BE DOSE ADJUSTED? | -TRADJENTA -NO BECAUSE MOST ELIMINATED IN FECES |
| ALOGLIPTIN BRAND NAME? | NESINA |
| ALPHA GLUCOSIDASE INHIBITORS PREVENT THE HYDROLYSIS OF CARBOHYDRATES TRUE OR FALSE? | TRUE |
| ACARBOSE BRAND NAME | PRECOSE |
| MIGLITOL BRAND NAME | GLYSET |
| WHERE DO SGLT2 WORK? HOW DO THEY WORK? | -KIDNEYS - BLOCK THE EABSORPTION OF SODIUM AND GLUCOSE AND EXCRETES IT IN URINE |
| WHAT IS THE LEAD MOLECULE FOR SGLT2 | PHORIZIN |
| HOW MANY CARBONS DOES GLUCOSE CONTAIN? | 6 |
| SGLT2 EFFECTS? | -WEIGHT LOSS -UTI -PLYURIA -GENITOURINARY INFECTION |
| SGLT2 MORE SEVERE SIDE EFFECT | KETOACIDOSIS |
| CANAGLIFLOZIN BRAND NAME | INVOKANA |
| DAPAGLIFLOZIN BRAND NAME | FARXIGA |
| WHAT STRUCTURE DO ALL SGLT2 HAVE? | MODIFIED GLUCOSE |
| EMPAGLIFLOZIN BRAND NAME | JARDIANCE |
| ERTUGLIFLOZIN BRAND NAME | STEGLATRO |
| WHAT TYPE OF METABOLISM DO SGTL2 UNDERGO? WHERE ON THE STRUCTURE? | -O-GLUCURONIDATION -SUGAR |
| SGLT2 CAN BE USED FOR HF TRUE OR FALSE | TRUE |
| WHICH SGTL2 INHIBITOR REDUCE THE RISK OF HEART FAILURE? | SOTAGLIFLOZIN |
| SGLT2 CAN BE USED FOR HF TRUE OR FALSE | TRUE |
| WHICH SGTL2 INHIBITOR REDUCE THE RISK OF HEART FAILURE? | SOTAGLIFLOZIN |
Created by:
maarment