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PDAT2 > 9 - DM MedChem + Pharmacology > Flashcards

9 - DM MedChem + Pharmacology Flashcards

1
Q

Wut dis is

A

Meglitinides

insulin SECRETAGOGUES

  • *Repaglinide / Nateglinide**
  • less hypoGlycemia than sulfonylureas*
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2
Q

wut dis is

A

DPP-4 INHIBITORS

LASS

Linagliptin - Tradjenta

Alogliptin - Nesina

Sitagliptin - Januvia

Saxagliptin - Onglyza

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3
Q

Additives for

Short Acting Insulin

A

“humulin R / novolin R”

  • *Soluble Crystalline ZINC insulin**
  • nothing else*

Effect in <30 minutes

PEAK = 2-3 hours

Lasts = 5-8 Hours

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4
Q

SGLT-2 Inhibitors

MoA / AE

C-D-E-E- gliflozin

invokana = canagliflozin

A

Inhibit the sodium-glucose cotransporter 2 (SGLT2) in kidney

Blocking the reabsorption of glucose

allowing for the glucose to pass into the URINE

SGLT2 = main site of glucose reabsorption in the kidney

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5
Q

Sulfonylurea

SIDE EFFECTS + Drug Interactions

Glipizide + Glimepiride + Glyburide

A

hypoGlycemia
from too much GLUT4 taking in too much glucose

Metabolized by Liver -> excreted in kidney

Serum protein binding is HIGH

so it interacts with other HIGHLY PROTEIN BOUND DRUGS

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6
Q

Wut dis is?

A

BIGUANIDE

Metformin

BI = two of the same thang, litta N’s

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7
Q

Alpha Glucosidase Inhibitor

MoA

A
  • Hydrolyses Oligosaccharides -> smaller Monosacharides
    • which are absorbed in the GI TRACT
  • Delay Digestion of Ingested Carbs
    • Reducing POSTPRANDIAL Blood Glucose conc.
  • ​Glucose levels then rise more SLOWLY
    • LESS insulin response is required
  • Do not stimulate Insulin release
    • ​so they do not result in hypoglycemia
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8
Q

wut dis is

A

Alpha-Glucosidase Inhibitors

ACARBOSE

Miglitol / Voglibose

Look like glucose ay ay

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9
Q

Meglitinides

MoA + SAR

Repaglinide + Nateglinide

A

Pancreatic Insulin Release = INSULIN SECRETAGOGUE

similar to Sulfonylureas

2 binding sites same as Sulfonylurea

+

1 Unique binding site

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10
Q

How is Insulin

Chemically Degradated?

A

NEUTRAL pH –> Deamination@ ASNB3

Acidic Conditions–>Deamination (rxn with water)

Oxidation of S-S Bridges –> aggregation / protein structure loss

INSULINASE = cleaves disulfide linkages in BLOOD

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11
Q

Rapid Acting Insulin Products

A

LISPRO

ASPART

GLULISINE

(LAG)

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12
Q

GLP-1 Receptor Agonists

MoA + Function

Liraglutide = Victoza / Dulaglutide = Trulicity

Exanatide / albiglutide

A

Incretin-Based Therapy
secreted in response to a meal, mostly by endocrine L-cells in small intestine

Stimulates first phase release of insulin from pancreatic beta cells

FA’s promote albumin binding & limits the DPP4 degradation

Glucagon Secretion / Gastric Emptying / Appetite

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13
Q

Alpha-Glucosidase Inhibitors

AE + Drug Interactions

Acarbose + Miglitol + Voglibase

A

Carbs are SITTING IN THE GUT –> GI Issues

Flatuelence + Diarrhea + Abdominal Pain

from appearance of undigested cabs in the colon

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14
Q

What FACTORS affect the

Onset / degree / duration of action

of Insulin?

A

Primary Protein Structure
ANY change in the AA residues @ N/C-terminus of B-chain

Insulin CRYSTAL type
soluble/amorphous / crystal / microcrystal

ZINC OR PROTAMINE

Site of Injection
abdomen / upper arm / thigh / buttock

Smoker / Temp / Exercise Etc.

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15
Q

DPP4 Inhibitors

MoA + SAR

L-A-S-S -gliptin

A

_*slows the inhibition* of GLP-1_

MORE INCRETIN FUNCTION

reduce / slow down

Glucagon Secretion / Gastric Emptying / Appetite

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16
Q

Insulin Analog Creation

What do we make ADJUSTMENTS TO?

A
  • We make adjustments to the C-Terminus of the B-Chain
    • ​do not change Biological activity or immunogenicity
    • Influence the rate of dimer formation & or Seperation
      • ​​​All produced by RECOMBINANT DNA methods
17
Q

wut dis is

A

SGLT2 INHIBITOR
Sodium-Glucose Cotransport Inhibitors

C-D-E-E - GLIFLOZIN

CANA / DAPA / EMPA / ERTU

Invokana / Farxiga / Jardiance / Steglatro

looks like the Alpha Glucosidase inhibitor but with MORE

18
Q

TZDs

Side Effects + DI’s

Pioglitazone + Rosiglitazone

A
  • *HEPATIC TOXICITY**
  • similar to APAP*

Extensive P450 metabolism –>
metabolites excreted in URINE

PIOGLITAZONE decreases the
level of ESTROGEN oral contraceptives

19
Q

Long-Acting Insulin Products

A

Detemir

Glargine

Degludec

(DDG)

20
Q

wut dis is

A

TZDs

Rosiglitazone

Pioglitazone

TZD = THI-AZOLE

azole = Nitrogen 5 group + thi = sulfur too

21
Q

Meglitinides

Side Effects / DI’s

Repaglinide + Nateglinide

A

LESS hypoGlycemia than sulfonylureas

Short acting / immediately taken before meals

metabolized by CYP3A4

Nateglinide is CYP3A4 + CYP2C9, less drug interactions

22
Q

General changes on

Rapid Acting Insulin Analogs

A

L-A-G

c-terminus of B chain

Steric Hinderance / Charge-Repulsion

Reduced Self-Association

Absorbed MORE Rapily than regular insulin

23
Q

General Changes on

Long-Acting Insulin Analogues

(Basal insulin)

A

GG-DD, c-terminus of B chain

Increased Self-Aggregation in SC tissue

Reversible Albumin Binding

Crystalline depot –> low levels of circuling insulin

ULTRALENTE

Zinc Insulin forming LARGE particles

delayed onset + prolonged duration of action

24
Q

Alpha-Glucosidase Inhibitors

MoA + SAR

Acarbose + Miglitol + Voglibase

A

Alpha glucosidase normally hydrolyses oligosaccharides –> monosaccharides​ which get absorbed from the GI tract

  • DELAY* Digestion of CARBOHYDRATES
  • REDUCING* PostPandial Blood Glucose (PPG)

SPREADS OUT the release of Glucose –> less insulin response required

DO NOT stimulate insulin release, no hypoglycemia

25
Q

Wut dis is?

A

SULFONYLUREA

Glipizide / Glimepiride / Glyburide

SULFON = Sulfur + 2 Oxygens

UREA = 2N-C=O

26
Q

Biguanides

MoA + SAR

Metformin (glucophage)

A

Discovered from a PLANT = Goat’s Rue

only hypoglycemic shown to REDUCE CV MORTALITY

  • *Reduces Plasma Glucose**
  • does NOT promote insulin secretion, needs INSULIN to be present*

RAISES levels of AMP –> stimulates AMPK –> numerous downstream effects:

  • *reduction of HYPERlipidemia**
  • *hepatic glucose production**
27
Q

Additives for

Intermediate-Acting Insulin

Isophane NPH Insulin

A

“Humulin N / Novolin N”

Suspension of Crystalline Zinc Insulin + PROTAMINE

Action of NPH is HIGHLY UNPREDICTABLE

variability of absorption >50%

28
Q

Biguanides

Side Effects + Drug Interactions

Metformin (glucophage)

A

low risk of _hypoGlycemia_**, does NOT promote insulin secretion

Severe LACTIC ACIDOSIS, rare but potential

not metabolized –> urine/renal excretion

CIMETIDINE = competitive inhibitor of renal excretion

29
Q

Acarbose

(Precose)

Voglibose

A

α-Glucosidase Inhibitor

  • Delay the digestion of ingested carbohydrates,
    • reducing postprandial blood glucose concentrations
    • no DIRECT stimulation of insulin
  • Obtained from MICROBIAL cultures
    • ​Poorly absorbed
      • remains in the intestinal LUMEN
  • Side effects: Flatulence / Diarrhea / Abdominal Pain
30
Q

Miglitol

(Glyset)

A

α-Glucosidase Inhibitor

31
Q

α-Glucosidase Inhibitors

Adverse Effects

A
  • Appearance of undigested carbohydrates in COLON​
    • Diarrhea
    • Flatulance
    • Abdominal Pain
32
Q

Sulfonylurea

MoA + SAR

Glipizide + Glimepiride + Glyburide

A

inhibit/block Kir 6.2 = ATP-sensitive Potassium Channel
on Pancreatic B-Cells

  • Sulfonylurea –/–> Potassium channel
    • DEPOLARIZATION
      • –> Opening of Calcium Channels ^^CA2+
        • Insulin Secretion
          • insulin secretagogue & insulin receptor sensitivity
33
Q

TZDs

MoA + SAR

Pioglitazone + Rosiglitazone

actos + avandia

A

Insulin SENSITIZERS

Acts on PPAR-Y to activate insulin-responsive genes that regulate carb + lipid metabolism

Gives INCREASED Insulin Sensitivity in
adipocytes / hepatocytes / skeletal muscle

34
Q

Intermediate - Acting Insulin

A

NPH = Neutral Protamine Hagedorn Insulin

Isophane NPH Insulin

35
Q

What drug types are

INSULIN SECRETAGOGUES?

A

SULFONYLUREAS

Glipizide + Glyburide + Glyburide

MEGLITINIDES
Repaniglide + Nateglinide

increased risk of hypoGlycemia

metformin too but does not have hypoglycemia issue

36
Q

Amylin Analogues

MoA / Function

Pramlintide = Symlin

A

Amylin is co-secreted with insulin from beta cells, in response to meals

Amylin Functions:

  • SLOWS* Gastric Emptying
  • Lower BG levels by DECREASING* Glucagon Release

PDAT2 (22 decks)

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