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PDAT2 > 9 - DM MedChem + Pharmacology > Flashcards

9 - DM MedChem + Pharmacology Flashcards

(36 cards)

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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?

Study These Flashcards
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

Study These Flashcards
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

Study These Flashcards
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

Study These Flashcards
A

Detemir

Glargine

Degludec

(DDG)

20
Q

wut dis is

Study These Flashcards
A

TZDs

Rosiglitazone

Pioglitazone

TZD = THI-AZOLE

azole = Nitrogen 5 group + thi = sulfur too

21
Q

Meglitinides

Side Effects / DI’s

Repaglinide + Nateglinide

Study These Flashcards
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

Study These Flashcards
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)

Study These Flashcards
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

Study These Flashcards
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
**Wut dis is?**
**_SULFONYLUREA_** Glipizide / Glimepiride / Glyburide **SULFON = Sulfur + 2 Oxygens** **UREA = 2N-C=O**
26
**Biguanides** **MoA + SAR** **Metformin (glucophage)**
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
**Additives for** **_Intermediate-Acting Insulin_** _Isophane NPH Insulin_
"Humulin N / Novolin N" Suspension of **Crystalline Zinc Insulin + _PROTAMINE_** Action of **NPH** is ***HIGHLY UNPREDICTABLE*** *variability of absorption **\>50%***
28
**Biguanides** **Side Effects + Drug Interactions** **Metformin (glucophage)**
*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
**Acarbose** (Precose) ***Voglibose***
**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
**Miglitol** | (Glyset)
**α-Glucosidase Inhibitor**
31
**α-Glucosidase Inhibitors** ***Adverse Effects***
* Appearance of **undigested carbohydrates in COLON****​** * **Diarrhea** * **Flatulance** * **Abdominal Pain**
32
**Sulfonylurea** **MoA + SAR** Glipizide + Glimepiride + Glyburide
*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
**TZDs** **MoA + SAR** Pioglitazone + Rosiglitazone actos + avandia
**_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
**Intermediate - Acting Insulin**
**NPH = Neutral Protamine Hagedorn Insulin** **Isophane NPH Insulin**
35
**What drug types are** **INSULIN SECRETAGOGUES?**
**_SULFONYLUREAS_** Glipizide + Glyburide + Glyburide **_MEGLITINIDES_** Repaniglide + Nateglinide _increased risk of **hypoGlycemia**_ *metformin too but does not have hypoglycemia issue*
36
**Amylin Analogues** **MoA / Function** **Pramlintide = Symlin**
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_**

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