Newer Anti-Diabetic Drugs

NEWER ANTI-DIABETIC DRUGS

Q. 1

All are true about Exenatide except ‑

 A >Decreases glucagon secretion
 B

It is GLPI analogue

 C >Used in type 1 DM
 D >Given subcutaneously
Q. 1

All are true about Exenatide except ‑

 A >Decreases glucagon secretion
 B

It is GLPI analogue

 C >Used in type 1 DM
 D >Given subcutaneously
Ans. C

Explanation:

Used in type I diabetes mellitus [Ref: Katzung 11/e p. 745; Harrison I7/e p 2301; KDT 6/e p 273]

  • Exenatide belongs to class of drugs called “incretins”.
  • Incretins are insulin stimulation hypoglycemic factor found in the duodenum.

– Incretin hormones are produced in the gastrointestinal tract in response to nutrient entry. Incretins, in turn, stimulate insulin, secretion.

Glucagon like polypeptide (GLP-1) and gastric inhibitory polypeptide (GIP) are two examples of incretins.

  • Glucagon like peptide (GLP-1) is a naturally occurring peptide that enhances insulin secretion in response to raised plasma glucose concentrations. It can lower blood glucose level by other methods too.
  • It does so by: ?

– Increasing the secretion of insulin from the pancreas.

– Slows absorption of glucose from the gut.

– Reduces the action of glucagon (Glucagon increases glucose production by liver).

  • These actions of GLP-1 lead to lowering of blood sugar levels.
  • Thus, the compound has unique properties to reduce postprandial glucose level.
  • But these properties are offset by very important adverse effect.

GLP-1 is rapidly (1-2 minutes) deactivated by the dipeptidyl peptidase IV DPP (IV) enzyme.

  • Thus GLP-1 must be infused continuously to have therapeutic benefits.
  • Consequently, considerable work has been performed to produce GLP- 1 receptor agonist that maintain the physiological effects of native incretin but are resistant to the action of DPP IV.
  • Exenatide is a synthetic GLP-1 receptor agonist that is resistant to DPP-IV and has full agonistic activity for GLP-1 receptors.
  • Exenatide is approved only for use as an adjunctive therapy to improve glycemic control in patients with type 2 diabetes mellitus who are taking metformin, sulfonylurea or a combination of both hut have not achieved adequate glycemic control.

-This drug is effective in lowering glycosylated hemoglobin concentration and promotes weight loss in type 2 diabetes mellitus.

  • Exenatide is injected “subcutaneously” within 60 minutes before meal.

– When exenatide is added to preexisting sulfottylurea therapy the oral hypoglycemic dosage should be reduced to prevent hypoglycemia.


Q. 2

After a meal rich in carbohydrate, insulin secretion is stimulated by

 A

CCK

 B

Serotonin

 C

VIP

 D

GLP-1 (7-36) amide

Q. 2

After a meal rich in carbohydrate, insulin secretion is stimulated by

 A

CCK

 B

Serotonin

 C

VIP

 D

GLP-1 (7-36) amide

Ans. D

Explanation:

D i.e. GLP-1 (7-36) amide


Q. 3

All are true about Exenatide except –

 A

Decreases glucagon secretion

 B

It is GLP 1 analogue

 C

Used in type 1 DM

 D

Given subcutaneously

Q. 3

All are true about Exenatide except –

 A

Decreases glucagon secretion

 B

It is GLP 1 analogue

 C

Used in type 1 DM

 D

Given subcutaneously

Ans. C

Explanation:

Ans. is ‘c’ i.e., Used in type I diabetes mellitus

Exenatide is a synthetic glucagon-like peptide -1 (GLP-l) analogue.

o It acts similar to GLP-1 —> Enhancement of postprandial insulin release, suppression of glucagon release and appetite as well as slowing of gastric emptying.

o It is given by subcutaneous route & used in type 2 DM

Quiz In Between


Q. 4

Amylin is secreted by ‑

 A

α-cells of pancreas

 B

β-cells of pancreas

 C

δ-cells of pancreas

 D

None

Q. 4

Amylin is secreted by ‑

 A

α-cells of pancreas

 B

β-cells of pancreas

 C

δ-cells of pancreas

 D

None

Ans. B

Explanation:

Ans. is ‘b’ i.e.,β-cells of pancreas

Pancreas is a structure which may be considered two organs in one : Exocrine pancreas and endocrine pancreas.

Its exocrine part secretes digestive enzymes and has been discussed in respective chapter.

The endocrine part, which secretes hormone will be discussed here.

The endocrine part forms only about 1% of weight of pancreas.

Histologically, the endocrine pancreas is formed by about a million of pancreatic islets (islets of langerhans).

The islets have four types of cells which secrete four different hormones.

i) A cells form about 25% of the islet cells and secrete glucagon.

ii) B cells form about 70% of the islet cells and secrete insulin and amylin.

iii) D cells form about 5% of the islet cells and secrete somatostatin.

iv) F cells are very few in number and secrete pancreatic polypeptide.


Q. 5

Effect of GLP-1 ‑

 A

Increased aldosterone secretion by adrenal

 B

Increased PTH secretion

 C

Increased insulin secretion from beta-cells of pancreas

 D

Increased testosterone secretion from Leydig cells

Q. 5

Effect of GLP-1 ‑

 A

Increased aldosterone secretion by adrenal

 B

Increased PTH secretion

 C

Increased insulin secretion from beta-cells of pancreas

 D

Increased testosterone secretion from Leydig cells

Ans. C

Explanation:

Ans. is ‘c’ i.e., Increased insulin secretion from beta-cells of pancreas


Q. 6

Bromocriptine is used in following clinical situations except ‑

 A

Type II DM

 B

Hepatic Coma

 C

Cyclical mastalgia

 D

Hypoprolactinemia

Q. 6

Bromocriptine is used in following clinical situations except ‑

 A

Type II DM

 B

Hepatic Coma

 C

Cyclical mastalgia

 D

Hypoprolactinemia

Ans. D

Explanation:

Ans. is `d’ i.e., Hypoprolactinemia

Uses of Bromocriptive

  • Bromocriptine is a powerful dopamine agonist. It suppresses prolactin secretion while promoting secretion of gonadotropins.
  • Its therapeutic uses are:
  1. Suppression of lactation in galactorrhea
  2. Cyclical mastalgia
  3. Induction of ovulation in anovulatory infertility caused by hyperprolactinemia
  4. Parkinsonism
  5. Acromegaly due to small pitutary tumours
  6. Hepatic coma
  7. Recently, it has been approved for treatment of type 2 DM.

Quiz In Between


Q. 7

Pramlintide is ‑

 A

Synthetic amylin analogue

 B

Inhibitor of DPP 4

 C

GLP 1 analogue

 D

PPAR gamma

Q. 7

Pramlintide is ‑

 A

Synthetic amylin analogue

 B

Inhibitor of DPP 4

 C

GLP 1 analogue

 D

PPAR gamma

Ans. A

Explanation:

Ans. is ‘a’ i.e., Synthetic amylin analogue

NEWER ANTIDIABETIC DRUGS

Exenatide

  • Exenatide is a synthetic glucagon-like peptide – 1 (GLP-1) analogue.
  • GLP-1 is an important incretin that is released from gut in response to oral glucose.
  • But GLP-1 can not be used clinically as it is degraded rapidly by enzyme dipeptidly peptidase → (DPP-4). 
  • Exenatide is resistant to DPP-4.
  • It acts similar to GLP-1 → Enhancement of postprandial insulin release, suppression of glucagon release and appetite as well as slowing of gastric emptying.
  • It is given by subcutaneous route & used in type 2 DM
  • Nausea is most important side effect.

Sitagliptin

  • This is orally active inhibitor of DPP-4.
  • It prevents degradation of endogenous GLP-1 and other incretins, potentiating their action, resulting in limitation of postprandial hyperglycemia.
  • It is used in type 2 DM.
  • Other DPP-4 inhibitor is vildagliptin

Pramlintide

  • This is a synthetic amylin analogue (Amylin is a polypeptide produced by pancreatic (3-cells which reduces glucagon secretion from a-cells and delays gastric emptying).
  • Pramlintide attenuates postprandial hyperglycemia and exerts a centrally mediate anorectic action. o It is given by subcutaneous route and is used in both Type 1 and Type 2 DM.

Glucomannan

  • This is powdered extract from tuber of konjar.
  • It is promoted as a dietary adjunct for diabetes.
  • It swells in stomach by absorbing water and is claimed to reduce appetite, blood sugar, serum lipids and relieve constipation.

Bromocriptine

  • Recently bromocriptine has been approved by FDA, as an adjunct to diet and exercise to improve glycemic control in type 2 DM. It has been found that dopamine alter insulin resistance by acting on hypothalmus and bromocriptine blocks O2 receptors.

Q. 8

Incretin like function is seen in ‑

 A

Exenatide

 B

Miglital

 C

Poiglitazone

 D

Repaglinide

Q. 8

Incretin like function is seen in ‑

 A

Exenatide

 B

Miglital

 C

Poiglitazone

 D

Repaglinide

Ans. A

Explanation:

Ans. is ‘a’ i.e., Exenatide

Exenatide is a synthetic glucagon-like peptide – 1 (GLP-1) analogue.

GLP-1 is an important incretin that is released from gut in response to oral glucose.

But GLP-1 can not be used clinically as it is degraded rapidly by enzyme dipeptidly peptidase → (DPP-4).

Exenatide is resistant to DPP-4.

It acts similar to GLP-1 → Enhancement of postprandial insulin release, suppression of glucagon release and appetite as well as slowing of gastric emptying.

It is given by subcutaneous route & used in type 2 DM

Nausea is most important side effect.


Q. 9

True about sitagliptin is all except 

 A

Used in type II DM

 B

 Used in combination with other oral hypoglycaemic

 C

Cannot be used orally

 D

 All are true

Q. 9

True about sitagliptin is all except 

 A

Used in type II DM

 B

 Used in combination with other oral hypoglycaemic

 C

Cannot be used orally

 D

 All are true

Ans. C

Explanation:

Ans. is ‘c’ i.e., Cannot be used orally 

Sitagliptin

  • This is orally active inhibitor of DPP-4.
  • It prevents degradation of endogenous GLP- 1 and other incretins, potentiating their action, resulting in limitation of postprandial hyperglycemia.
  • It is used in type 2 DM.
  • Other DPP-4 inhibitor is vildagliptin.

Quiz In Between


Q. 10

In which condition, Dapagliflozin is used?

 A
Type 1 diabetes
 B

Breast cancer

 C

Type 2 diabetes.

 D

Bladder cancer

Q. 10

In which condition, Dapagliflozin is used?

 A
Type 1 diabetes
 B

Breast cancer

 C

Type 2 diabetes.

 D

Bladder cancer

Ans. C

Explanation:

Type 2 diabetes.

DAPAGLIFLOZIN

  • An SGLT-2 inhibitor drug of gliflozin class.
  • Used in type 2 diabetes treatment. 
MECHANISM OF ACTION:
  • Glucose is reabsorbed completely in proximal tubules by sodium-glucose cotransporter-2 [SGLT-2]. 
  • Dapagliflozin acts by inhibiting SGLT-2 transporter.

Q. 11

Dapagliflozin inhibits which glucose transporter?

 A

GLUT – 3

 B

GLUT – 1

 C

SGLT-2 

 D

GLUT – 2

Q. 11

Dapagliflozin inhibits which glucose transporter?

 A

GLUT – 3

 B

GLUT – 1

 C

SGLT-2 

 D

GLUT – 2

Ans. C

Explanation:

SGLT-2.

DAPAGLIFLOZIN

  • An SGLT-2 inhibitor drug of gliflozin class.
  • Used in type 2 diabetes treatment. 
MECHANISM OF ACTION:
  • Glucose is reabsorbed completely in proximal tubules by sodium-glucose cotransporter-2 [SGLT-2]. 
  • Dapagliflozin acts by inhibiting SGLT-2 transporter.

Q. 12

Which is the most common side effect of Dapagliflozin?

 A

Glycosuria 

 B

Weight loss

 C

Fatigue

 D

All of the above

Q. 12

Which is the most common side effect of Dapagliflozin?

 A

Glycosuria 

 B

Weight loss

 C

Fatigue

 D

All of the above

Ans. D

Explanation:

Causes all of the effects.

DAPAGLIFLOZIN

  • An SGLT-2 inhibitor drug of gliflozin class.
  • Used in type 2 diabetes treatment. 
MECHANISM OF ACTION:
  • Glucose is reabsorbed completely in proximal tubules by sodium-glucose cotransporter-2 [SGLT-2]. 
  • Dapagliflozin acts by inhibiting SGLT-2 transporter.
Effects:
  • Single daily dose produces round-the-clock glucosuria lowering blood glucose levels.

SIDE EFFECTS:

  • Main effects:
    • Heavy glycosuria (Up to 70 grams/day).
      • Causes rapid weight loss & tiredness.
    • Increased incidence of urinary tract infections & genital infections (candidiasis).
      • Because increased urinary glucose worsens infections already associated with diabetes.
    • Increased risk of diabetic ketoacidosis.
    • Increased urinary frequency.
  • Other effects:
    • Decreases bone mineral density —-> Increases risk of fractures.
    • Higher rates of breast & bladder cancers reported.
    • Hypotensive reactions.

Quiz In Between



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