ANTI-DIABETIC DRUGS Flashcards

1
Q

Diabetes mellitus (DM) is defined as a ______geneous metabolic disorder characterized by (acute or chronic?) ______glycemia with relative disturbance of ————,________,________

A

heterogeneous

chronic

hyperglycemia

carbohydrate, fat and protein metabolism

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2
Q

There are two major types of DM and a number of minor types
Major types
Type 1/ _______ Dependent DM
Type 2/ __________ Dependent DM

Minor types
•____________ DM
•_______ Onset Diabetes of the _______
•_____________ DM

A

Insulin

Non Insulin

Gestational DM

Maturity ; Young

Secondary DM

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3
Q

PATHOPHYSIOLOGY

In a normal patient, Glucose metabolism is regulated by the hormone _________
And this is a polypeptide hormone made up of _____ amino acids

It is produced in the _________ Cells of the _________

It is secreted into circulation usually in response to _____ease in Glucose in the _________, usually (before or after?) a meal

A

INSULIN

51 amino acids

Beta Islet ; Pancreas

increase ; blood ; after

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4
Q

Function of Insulin after release includes

Enables _________ by tissues in the body

___________ Glycogen synthesis

___________ Gluconeogenesis and Glycogenolysis

___________ Lipogenesis

___________ Lipolysis

___________ Protein ______bolism

A

Glucose uptake

Stimulates

Inhibits

Stimulates

Inhibits

Stimulates

Anabolism

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5
Q

Hence absence or inactivity of Insulin would lead to

(Reduced or Increased ?) Uptake of Glucose by Tissues

(Reduced or Increased ?) Hepatic Glycogenosis and Gluconeogenesis

(Reduced or Increased ?) Lipolysis

(Reduced or Increased ?) Protein Catabolism

(Reduced or Increased ?) uptake of Glucose by tissues leads to accumulation of Glucose in the blood

Thus (ACUTE or CHRONIC?) HYPERGLYCEMIA

A

Reduced
Increased
Increased
Increased
Reduced

CHRONIC HYPERGLYCEMIA

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6
Q

ETIOLOGY

Type I Insulin-dependent diabetes mellitus (IDDM)

There is ____________ in pancreatic _______;

____________ (type _____) antibodies that ___________ are detectable in blood.

_________ INSULIN DEFICIENCY from ______

A

β cell destruction ; islets

Autoimmune (type 1A)

destroy β cells

Absolute; start

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7
Q

Type II Noninsulin-dependent diabetes mellitus (NIDDM)
Reduced ________ of ________ to ______ or ________

________ INSULIN DEFICIENCY at ______ stage

A

sensitivity ; peripheral tissues

insulin ; Insulin resistance

Relative ; later stage

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8
Q

Classification of hypoglycemic agents

A and B

B can be divided into C and D

A can be divided into E, F , G

A

A parenteral
B oral
C sulfonylureas
D Biguanides
E short acting
F intermediate acting
G long acting

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9
Q

INSULINS

Rapid
Insulin _______
Insulin _______
Insulin _______

Short acting
_______ Insulin

Intermediate acting
Neutral protamine Hagedorn/Insulin _______

Long acting
Insulin _______
Insulin _______

A

Rapid
Insulin Lipro
Insulin Aspart Insulin Glulisine

Short acting
Regular Insulin

Intermediate acting
Neutral protamine Hagedorn/Insulin isophane

Long acting
Insulin glargine
Insulin detemir

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10
Q

INSULIN

SOURCE

Naturally
Extracted from ______

– Artificially
Produced by ___________ technology using special strains of ___________ or _________ that have been genetically altered to ______________________________

A

PIGS

recombinant DNA technology

Escherichia coli ; yeast

contain the gene for human insulin

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11
Q

INSULIN

Binds to Insulin Receptor in the __________, __________ and __________

Insulin receptors are a type of __________ RECEPTOR

Activation of this receptor leads to the expression of unique glucose transporters on the membrane of the cells called __________

_______ expression causes an uptake of GLUCOSE from the blood

A

LIVER, SKELETAL MUSCLE and ADIPOSE TISSUE

TYROSINE KINASE RECEPTOR

GLUT; GLUT

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12
Q

INSULIN: PHARMACOKINETICS

Administered _____________

Insulin preparations vary primarily based on
________ and _____________

Metabolized in the _____ and _______ by _____________ ENZYME/ _____________

A

SUBCUTANEOUSLY

Onset; Duration of action

Liver and Kidney

INSULIN-DEGRADING ENZYME/ INSULIN PROTEASE

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13
Q

INSULIN: ADVERSE EFFECT

_____________
Weight _____
____________ at injection site
______kalemia
______/ _________ reaction
Edema
______ and _________ at Injection site

A

Hypoglycemia; gain

Lipodystrophy ; Hypokalemia

Allergic/ Hypersensitivity

Pain and Erythema

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14
Q

NON-Insulins

Insulin Secretagogues
____________
____________

Insulin Sensitizer

____________
____________/____________

Glucosidase Inhibitors
____________
____________

A

Meglitinide
Sulfonylurea

Biguanides
Thiazolidinediones/Glitazone

Acarbose
Miglitol

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15
Q

NON-Insulins

Insulin ________

Insulin _________

_________ Inhibitors

___________ Inhibitor

________ analogue

__________ ________

A

Secretagogues

Sensitizer

Glucosidase

Dipeptidyl Peptidase IV

Amylin

Incretin mimetic

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16
Q

NON-INSULINS

Dipeptidyl Peptidase IV Inhibitor
___________

Amylin analogue
__________

Incretin mimetic
___________

A

Sitagliptin

Pramlintide

Exenatide

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17
Q

Non-insulins: sulfonylureas

Examples

First Generation
___________
___________
___________

Second Generation
___________
___________
___________

A

Chlorpropamide
Tolbutamide
Acetohexamide

Glyburide
Glipizide
Glimepiride

18
Q

Mechanism of action of SULFONYLUREAS

Insulin __________

Binds and Block ______________________________ of the pancreatic β cells

This causes _________ of the cell membrane

Leading to ___________

Eventually causing ____________

Extra-pancreatic effect: ↓ ______ ___________, ↑ peripheral ____ ___________

A

Insulin secretagogue

ATP- sensitive potassium channels

depolarization ; calcium influx

Insulin secretion

hepatic gluconeogenesis ; insulin sensitivity

19
Q

Non-insulins : sulfonylureas

Adverse effect
________________
______ intolerance
Weight ______
______________ reaction
Granulocytopenic
_________ anemia

A

Hypoglycemia

Alcohol ; gain

Allergic skin

Hemolytic

20
Q

NON-INSULINS: MEGLITINIDES

Examples
__________;________

A

Repaglinide
Nateglinide

21
Q

NON-INSULINS: MEGLITINIDES

Mechanism of action

Insulin ___________
Binds and Block _______________of the pancreatic β cells
Causes _________ leading to ________________

Eventually causing Insulin _________

A

ATP-sensitive potassium channels

depolarization ;calcium influx

Insulin secretion

22
Q

NON-INSULINS: MEGLITINIDES

Adverse effect
______________
Weight ______
________toxicity

A

Hypoglycemia

gain

Hepato

23
Q

Non INSULINS: BIGUANIDES

Example

____________

A

Metformin

24
Q

Non INSULINS: BIGUANIDES

Mechanism of action
Reduction in insulin __________ via modification of ______________________

–Inhibits _______________________(mGPD)

•Increases peripheral insulin _________ → ↑ peripheral _________ and glycolysis

A

Insulin resistance

glucose metabolic pathways

mitochondrial glycerophosphate dehydrogenase

insulin sensitivity

glucose uptake

25
Q

NON-INSULINS: BIGUANIDES

Adverse effect

_________ ________
________/ _______ taste in the mouth
____________ deficiency
Weight ______

A

Lactic Acidosis

Dysgeusia/ Metallic taste in the mouth

Vitamin B12 deficiency

Weight loss

26
Q

NON-INSULINS: THIAZOLIDINEDIONES

Examples

List 3

A

Pioglitazone
Troglitazone
Rosiglitazone

27
Q

NON-INSULINS: THIAZOLIDINEDIONES

Mechanism of action
Bind and activates of the _________ factor ______ (_______________________________ of _______ type in the nucleus)

Lead to Increased glucose _________ and _____________ production

A

transcription

PPARγ

peroxisome proliferator-activated receptor

gamma

utilization

hepatic glucose production

28
Q

NON-INSULINS: THIAZOLIDINEDIONES

Adverse effect
Weight _____
Increase risk of _________
Increased risk of _________
Edema

A

gain; Heart failure

Bone fracture

29
Q

Non-INSULINS: INCRETIN MIMETICS

Examples
List 4

A

Exenatide
Liraglutide
Albiglutide
Dulaglutide

30
Q

Non-INSULINS: INCRETIN MIMETICS

Mechanism of action

Binds to ___________________ (______) receptor

Lead to increase Insulin _______ and decrease ________ secretion

A

Glucagon Like Peptide-1 (GLP1)

Insulin secretion

Glucagon secretion

31
Q

Non-INSULINS: INCRETIN MIMETICS

Adverse effect
Nausea
Vomiting
(Early or Late?) Satiety
___________
Weight ____

A

Early

Pancreatitis

Loss

32
Q

Non insulins : DIPEPTIDYL PEPTIDASE INHIBITOR

Examples
List 3

A

Sitagliptin
Saxagliptin
Linagliptin

33
Q

Non insulins : DIPEPTIDYL PEPTIDASE INHIBITOR

Mechanism of action
Binds and Inhibits the _____ enzymes that breaks down ______ or _______

Hence leads to ______________________

This leads to increase insulin _________ and decrease ________ secretion

A

DPP-4 enzymes

GLP-1 or Incretin

accumulation of Incretin

insulin secretion

glucagon secretion

34
Q

DIPEPTIDYL PEPTIDASE INHIBITOR
Adverse effect

___________ upset
Arthralgia
_____ satiety
Risk of _______ infection
Risk of _______itis
Risk of _________ infection
Risk of _______ failure
Headache
Dizziness

A

Gastrointestinal upset

Early satiety

Urinary infection

Pancreatitis

Respiratory infection

Renal failure

35
Q

Non-Insulins: GLUCOSIDASE INHIBITOR

Example

____________
_______________

A

Acarbose
Miglitol

36
Q

Non-Insulins: GLUCOSIDASE INHIBITOR

Mechanism of action

Binds and inhibit _______________ (a brush border enzyme expressed by _________________ cells

This causes delayed and decrease intestinal glucose _________
Hence reduces _________ after ________

A

alpha-glucosidase

intestinal epithelial cells

intestinal glucose absorption

hyperglycemia

food ingestion

37
Q

NON-insulins: GLUCOSIDASE INHIBITOR

Adverse effect
__________
_________
Abdominal _________
Diarrhea

A

Flatulence

Bloating

Abdominal discomfort

38
Q

Non-insulins: AMYLIN ANALGOUE

Examples
_______________

A

Pramlintide

39
Q

Non-insulins: AMYLIN ANALGOUE

Mechanism of action

Acting as an _______________

________ is a peptide hormone that is co-secreted with insulin

Hence pramlintide delays __________, decreases ________________ secretion, and improves ________.

A

amylinomimetic

Amylin

gastric emptying

postprandial glucagon

satiety

40
Q

AMYLIN ANALGOUE

Adverse effect
Nausea
Anorexia
Vomiting.

A

Lol

41
Q

Miscellaneous: GESTATIONAL DIABETES

__________
_____________
____________

A

Insulin
Glyburide
Metformin