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Drugs > Endocrine Drugs > Flashcards

Endocrine Drugs Flashcards

1
Q

Indication of sulphonylureas

A

Type 2 diabetes mellitus is with diet and exercise

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1
Q

Example of sulphonylureas

A

Gliclazide
Glimepiride
Tolbutamide

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2
Q

Mechanism of action of sulphonylureas

A
  • stimulates B cells of the pancreas to produce more insulin
  • increases cellular glucose uptake and glycogenesis; reduces gluconeogenesis
  • Binds to the high-affinity receptors on the ATP-sesnitve potassium (KATP) channells on B-islet cell plasma membranes, blocks resulting in Ca2+ entry and insulin release.
  • gliclazide is short acting (12hrs approx)
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3
Q

Patient information of sulphonylureas

A

Compliance important
Maintain consistent diet
Avoid alcohol

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4
Q

Side effects sulphonylureas

A 
Hypoglycaemia 
Rashes 
Vomiting 
Stomach pain
Indigestion 
Weight gain (not recommended as first choice in obese patients)
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5
Q

Example of biguanide

A

Metformin

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6
Q

Indication of biguanides

A

Type 2 DM along with diet and exercise

- metabolic and reproductive abnormalities with PCOS

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7
Q

Mechanism of action of biguanides

A
  • increases the activity of AMP dependent protein kinase (AMPK)
  • this inhibits hepatic gluconeogenesis
  • Increases glucose uptake and utilisation in skeletal muscle thereby reduces insulin resistance
  • does not increase insulin production therefore will not cause hypoglycaemia
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8
Q

Pharmacokinetics/ pharmacodynamics of biguanides

A
  • not recommended in pregnancy and renal failure (EGFR
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9
Q

Side effects of biguanides

A
  • diarrhoea
  • nausea and vomiting
  • taste disturbances (metallic taste)
  • lack of appetite
  • risk of lactic acidosis in patients with renal failure
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11
Q

Patient information for biguanides

A
  • take them at the same time everyday

- avoid alcohol

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12
Q

Example of thiazlidinediones

A

Pioglitazone

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13
Q

Mechanism of action of thiazolidinediones

A
  • Bind to a nuclear receptor (peroxisome proliferator-activated receptor gamma PPARy)
  • receptor complexed with retinoid X receptor
  • receptor found mainly in adipose tissue (may be found in muscle and liver) - increases peripheral insulin resistance
  • mediates differentiation of adipocytes, increases lipogenesis and enhances uptake of fatty acids + glucose (hyperinsulinaemia, hyperglycaemia, hypertriglycaeridaemia and HBA1c levels improved)
  • drug changes PPARy-RXR complex so that it binds DNA and promotes transcription of several genes important in insulin signalling
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14
Q

Indication of Thiazolidinediones

A

Type 2 Diabetes (single, dual or triple therapy)

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15
Q

Side effects of TZDs

A

GI distrubance
headaches
weight gain
Hepatotoxicity

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16
Q

Patient information of TZDs

A
  • Take with metformin or sulphonylureas

- Monitoring of LFTS recommended due to hepatotoxicity

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17
Q

The incretin effect

A

the increased stimulation of insulin secretion elicited by oral as compared with intravenous administration of glucose under similar plasma glucose levels.

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18
Q

Incretin hormones

A
  • glucagon-like peptide 1 (GLP-1)
    Gastric inhibitor peptide (GIP)

these hormones are rapidly inactivated by dipeptidyl peptidase-4 (DPP-4)

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19
Q

Type of Incretin effect Drugs

A
  1. Mimic hormone secretion (incretin mimics)

2. Inihbit inactivation hormone ( DPP-4 inhibitors

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20
Q

DPP-4 inhibitors

A
  • blocks the action of Didpeptidylpeptidase-4 enzyme that degrades incretin hormones, including glucago-like peptidde-1 (GLP-1) and glucose dependent insulinotropic polypeptide (GIP)
  • incretin hormones increase they synthesis and release of insulin from pancreatic B islet cells when blood glucose concentrations are normal or elevated
  • Thus DDP-4 inhibitors increase the level of incretins and subsequently the level of insulin
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21
Q

Example of DPP-4 inhibitor

A

Sitagliptin, vildagliptin

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22
Q

Indication of DPP-4 inhibitor

A

Type 2 Diabetes mellitus

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23
Q

Side effects of DPP-4 inhibitors

A

GI distrubance
Upper respiratory tract infections
peripheral oedema

24
Q

Pharmacokinetics/PD of DPP4 inhibitors

A
  • avoud in pregnancy and breastfeeding

- may cause increase in plasma digoxin concentrations

25
Q

Example of incretin mimic

A

GLP-1 agonists - exenatide

26
Q

Mechanism of action of incretin mimic

A
  • binds to and activates glucago-like peptide -1 (GLP-1) receptors,
  • results in increased synthesis and secretion of insulin from pancreatic B islet cells
  • action of exenatide is glucose-dependent therefore as plasma glucose fall, insulin secretion also reduces.
  • Exenatide also suppresses the inappropriate secretion of glucagon
27
Q

Indications for incretin mimics

A

Type 2 DM

28
Q

Side effects of incretin mimics

A

GI disturbance
weight loss (potential benefit)
hypoglycaemia
injecion site reactions

29
Q

PK/PD of incretin mimics

A

Exenatide may enhance the anticoagulant effect of warfarin

30
Q

Actions of GLP-1 and GIP

A

GLP-1 and GIP act on the beta cells to increase insulin production to increase glucose uptake by peripheral tisues and decrease hepatic glucose production
GLP-1 also acts via the alpha cells to decrease glucagon release therefore decreasing hepatic glucose produciton

31
Q

Example of SGLUT-2 inhibitor

A

Gliflozin

32
Q

Mechanism of action of Gluflozin

A

-SGLUTs are responsible for mediating glucose reabsorption
SGLUT-2 is primary expressed in the kidney in the epithelial cells of the PCT
- dapaglifizon is a SGLUT-2 competitive inhibitor that acts to decrease renal absorption of glucose, promoting glycosuria and decreased blood glucose concentration

33
Q

Synthesis of insulin

A
  1. Transcription of the insulin gene product and subsequent processing result in production of the full-length mRNA that encodes preproinsulin
  2. Together the leader sequence + the B, C and A domains constitute preproinsulin
  3. During translation of mRNA, leader sequence is cleaved in the lumen of the RER (rough endoplasmic reticulum)
  4. What remains is pro-insulin, which consists of B, C, A domains
  5. Beginning in the trans-golgi, proteases cleaves the pro-insulin at two sites
  6. Releasing the C peptide, + mature insulin molecule (contains A and B domains connected by disulphide bonds)
  7. The secretory granule contains equimolar amounts of insulin and the C peptide as well as smaller amounts of proinsulin
  8. Components are all released into the extracellular space
34
Q

Biphasic release of insulin

A

Insulin release is a biphasic process.

  • The initial amount of insulin released upon glucose absorption is dependent on the amounts available in storage.
  • Once depleted, a second phase of insulin release is initiated. This latter release is prolonged since insulin has to be synthesized, processed, and secreted for the duration of the increase of blood glucose. Furthermore, beta cells also have to regenerate the stores of insulin initially depleted in the fast response phase.
35
Q

Glucose triggering insulin release

A
  1. Glucose enters B cell through GLUT-2 receptor by facilitated diffusion. Amino acids enter through a different route
  2. In the presence of glucokinase, entering glucose undergoes glycolysis and raises ATP by phosphorylating ADP. Some amino acids also enter the citric acid cycle and produces similar changes in ATP and ADP. In both, ration of NADH/NAD+ ratio increases
  3. Increased ATP, Increased ADP/ATP ratio, Increased NADH/NAD+ ratio causes KATP channels to close
  4. Closure of K+ channel causes Vm to become more positive (depolarisation)
  5. Depolarisation activates voltage-gated Ca2+ channels to open
  6. Increased Ca2+ permeability leads to increased Ca2+ influx and increased intracellular free calcium , also evokes a calcium-induced-calcium release
  7. Elevated calcium leads to exocytosis and release into the blood of insulin contained within the secretory granules
36
Q

Short acting insulin

A

insulin aspart - novorapid

Soluble insulin- Actrapid

37
Q

Intermediate insulin

A

Isophane insulin (insulatard)

38
Q

Long acting insulin

A
  • Insulin glargine, inulin detemir
39
Q

Mechanism of action of exogenous insulin

A
  • exogenous insulin mimics the effects of endogenous insulin
  • increases glycogenesis in the liver, adipose tissue and skeletal muscle
  • reduces hepatic gluconeogenesis and glycoggenolysis
40
Q

Indications for insulin

A
  • DM

- Emergency management of hyperkaelamia

41
Q

Side effects of insulin

A
  • hypoglycaemia

- lipohypertrophy at sites of inject

42
Q

Type of insulin regimens

A

Basal bolus regimen - (short acting insulin with each meal and long acting insulin overnight)

Twice daily regimen - Short and intermediate acting insulin given twice a day)

43
Q

Ways insulin can be administered

A

pens

  • more convenient and easier to transport that traditional sringe
  • repeatedly more accurate dosages
  • easier to use for those with impairments in visial and fine motor skills
  • Less injection pain (as polished and coated needles are not dulled by insertion into a vial of insulin before a second insertion into the skin)
  • Can be used without being noticed

Continuous subcutaneous Insulin infusion

  • CSII or ‘pump therapy’ can potentially provide significant improvement in glycaemic control and quality of life for some people with Type 1 diabetes.
  • Pumps make it easier to achieve glucose control with less danger of severe and incapacitating hypoglycaemia. However, the efficacy of this compared to SMBG is still debatable.
  • Specific but infrequent complications of CSII therapy include reactions and occasionally infections at the cannula site, tube blockage and pump malfunction.
  • CSII therapy is expensive, incurring costs for batteries, reservoirs, infusion sets, insulin, lancets, test strips and glucometers.
44
Q

Examples of thionamides

A
  • Carbimazole

- Propylthiouracil

45
Q

Mechanism of action of carbimazole

A
  • Prodrug that ndergoes metabolism to the active metabolite, thiamazole
  • the latter inhibits the iodination of tyrosyl residues in thyroglobulin
  • this is mediated through the enzyme thyroperoxidase and it also inhibits the coupling of iodotyrosones
  • both actions inhibit thyyroid hormone production
46
Q

Propylthiouracil mechanism of action

A
  • inhibits the conversion of iodide to iodine which thereby interferes with the degradation of thyroglobulin and thereby reduces T3 and T4 production
47
Q

Indication of thionamides

A
  • hyperthyroidism
  • thyrotoxoxis
  • preparing patients for thyroid surgery
48
Q

Side effects of thionamides

A

Rash
agranulocytosis
sore throat

49
Q

Important PD/PK for thionamides

A
  • Carbimazole is rapidly metabolised to thiamazole. The mean peak plasma concentration occurs one hour
  • It crosses the placenta and can be found in breast milk
  • The effect of anti-thyroid drugs can take several weeks to occur so are usually prescribed alongside a beta-blocker to reduce symptoms of hyperthyroidism
50
Q

Patient information for thionamides

A
  • Compliance is important

- Regular blood checks will be needed to monitor treatment response and renal, hepatic function and full blood counts

51
Q

Levythyroxine mechanism of action

A
  • Thyroxine increases the metabolic rate of all tissues in the body
  • Synthetically prepared levo-isomer of thyroxine
  • Acts like T4 and gets converted to T3 in the liver and kidney
  • Maintain brain function, food metabolism, and body temperature, among other effects
52
Q

Indication of synthetic thyroid hromone

A
  • hypothyrodisim

- chronic lymphocytic thyroiditis

53
Q

Side effects of synthetic thyroid hormone

A
  • Chest pain
  • Coma
  • Diarrhoea
  • Tachycardia
  • Itching
  • Muscle cramps
54
Q

Important PK/PD of synthetic thyroid hormones

A
  • Primarily eliminated by the kidneys
  • Intravenous formulations are available
  • The half-life is long (6 to 7 days) so thyroid function should be rechecked 6 weeks after a dose adjustment
55
Q

Patient information on synthetic thyroid hormones

A

Take 30-60 minutes before breakfast

Drugs (8 decks)

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