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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5282_Библиотеки_им_академика_М_И_Перельмана
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General Information
135
Chapter
Hypoglycemic Agents
Hypoglycemic agents are used to reduce increased blood glucose levels to the normal level.
These drugs are also called anti-diabetic drugs.
Diabetes mellitus, commonly referred to as diabetes, is a metabolic disorder that results in
high blood glucose levels than normal for a prolonged period. Symptoms of high blood sugar
include frequent urination, increased thirst, and increased hunger. If left untreated, diabetes can
cause many complications. Acute complications can include diabetic ketoacidosis, hyperosmolar
hyperglycemic state, or death. Serious long-term complications include cardiovascular disease,
stroke, chronic kidney disease, foot ulcers, and damage to the eyes.
The most common types of diabetes is as follows:
Type 1 Diabetes
A chronic condition in which the pancreas produces little or no insulin.
Type 2 Diabetes
A chronic condition in which the pancreas produces enough insulin but the body does not
use it properly. This is called insulin resistance.
Gestational Diabetes
A condition in which high blood sugar levels occur pregnant women.
Prediabetes
A condition in which blood sugar is high but not enough to be considered as Type-2 diabetes.
Hypoglycemic agents are classified as follows:
(A) Insulin Preparations
Insulin is a peptide hormone produced by beta cells of the pancreatic islets of Langerhans. It
regulates the metabolism of carbohydrates, fats, and protein by promoting the absorption of
especially, glucose from the blood into the fat, liver and skeletal muscles.
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A Textbook of Pharmaceutical
Chemistry
(i) Rapid-acting insulin preparations
Insulin lispro (Humalog)
Insulin aspart (Novolog)
Insulin glutisine
(ii) Intermediate-acting insulin preparations
Insulin zinc suspension (Lente preparation)
Neutral Protamine or isophane insulin
(iii) Long-acting insulin preparations
Insulin glargine (Lantus optiset)
Insulin detemir
(iv) Short-acting insulin preparations
Regular insulin
(B) Oral Antidiabetics
(a) Enhance insulin secretion
K
ATP
channel blockers
(i) Sulfonylureas
Tolbutamide
Glibenclamide
Glipizide
Glimepiride
(ii) Phenylalanine analogues
Repaglinide
Nateglinide
(iii) Dipeptidyl peptidase-4 inhibitors
Sitagliptin
Vildagliptin
137
Hypoglycemic Agents
(b) Biguanides
Metformin
(c) Pioglitazone
(d) α- glucosidase inhibitors
Acarbose
Miglitol
Tolbutamide
Structure:
O
N
H
S
O
O
N
H
Chemical name: N-[(Butylamino)carbonyl]-4-methylbenzenesulfonamide.
Uses: As an antidiabetic agent, useful in the management of type-2 diabetes.
Formulation: Tablet.
Brand name: Rastinon.
Glibenclamide
Structure:
S
N
H
N
H
O
O
O
N
H
OO
Cl
Chemical name: 5-Chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-
methoxybenzamide.
Uses: As an antidiabetic agent in the management of type-2 diabetes.
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A Textbook of Pharmaceutical
Chemistry
Formulation: Tablet.
Brand name: Daonil.
Glipizide
Structure:
S
NH
NH
O
O
O
N
H
O
N
N
H
3
C
Chemical name: N-[4-(N-(Cyclohexylcarbomyl)sulfamoylphenethyl]-5-methylpyrazine-2-
carboxamide.
Uses: As an antidiabetic agent.
Formulation: Tablet.
Brand names: Glynase and Glide.
Metformin
Structure:
NH
2
H
NN
N
H
N
H
Chemical name: N,N-Dimethylimidodicarbonimidicdiamide.
Uses: As an antidiabetic agent to treat type-2 diabetes.
Formulation: Tablet.
Brand names: Glycomet and Glylipanage.
139
Hypoglycemic Agents
Pioglitazone
Structure:
O N
CH
3
S
HN
O
O
Chemical name: (RS)-5-{4-[2-(Ethylpyridin-2-yl)ethoxy]benzyl}-thiazolidine-2,4-dione
Uses: As an antidiabetic agent to lower blood glucose levels in the treatment of diabetes
mellitus type-2.
Formulation: Tablet.
Brand names: Pionorm and Piozone.
Note: Currently not prescribed due to the high risk of bladder cancer.
Approved New Drugs
Soliqua 100/33 (Insulin Glargine and Lixisenatide Injection)
Mechanism of action: It inhibits lipolysis and proteolysis, and enhances protein synthesis.
Lixisenatide is a GLP-1 receptor agonist that increases glucose-dependent insulin release,
decreases glucagon secretion. Mostly, it is used for the treatment of inadequately controlled type
II diabetes.
Xultophy 100/3.6 (Insulin Degludec and Liraglutide Injection)
Mechanism of action: It is a glucagon-like peptide-1 (GLP-1) receptor agonist that
increases glucose-dependent insulin release, decreases glucagon secretion, and slows gastric
emptying.
It is used in the treatment of inadequately controlled type II diabetes.
Qternmet XR (Dapagliflozin, Metformin Hydrochloride, Saxagliptin)
Mechanism of action: It stimulates AMP-activated protein kinase.
General Information
140
Chapter
Non-steroidal Anti-
inflammatory Agents
Non-steroidal anti-inflammatory drugs (NSAIDs) are the agents that together provide
analgesia (pain killer/reliever) and antipyretic (fever-reducing) effects and in higher doses anti-
inflammatory effects.
Inflammation is defined as a defensive but exaggerated local tissue reaction in response to
exogenous insult. It is a complex phenomenon comprising of biochemical as well as
immunological factors. It is recognized by the following symptoms:
1. Calor (Heat)
2. Tumor (Swelling)
3. Rubor (Redness)
4. Dolar (Pain)
Tissue damage initiates the local release of various chemotactic factors that provide directly
or indirectly the appearance of the mediators of pain and inflammation. These factors include.
(a) Amines: Histamine and serotonin.
(b) Proteases: Kalikrein, Plasmin.
(c) Prostaglandins
(d) Hageman factor
Most NSAIDs inhibit the activity of cyclooxygenase-1 (COX-1) and cyclooxygenase-2
(COX-2) enzymes and thereby the synthesis of prostaglandins and thromboxanes.
The pain-relieving and anti-inflammatory effects of NSAIDs are mainly due to inhibition of
COX-2 and their unwanted side effects are largely due to inhibition of COX-1.
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Non-steroidal Anti-inflammatory Agents
NSAID’s are classified as follows:
(a) Salicylates
Aspirin (Acetylsalicylic acid)
(b) Propionic acid derivatives
Ibuprofen
Naproxen
Ketoprofen
(c) Fenamate
Mephenamic acid
(d) Enolic acid derivatives
Piroxicam
(e) Acetic acid derivatives
Indomethacin
Ketorolac
(f) P-Amino phenol derivatives
Paracetamol (Acetaminophen)
(g) COX-II inhibitors
Nimesulide (Banned in certain countries due to its hepatotoxicity).
Diclofenac
Aceclofenac
Meloxicam
(h) Selective COX-II inhibitors
Celecoxib
Parecoxib
(i) Pyrazolone derivatives
Phenyl butazone
(j) Morphine analogs (Narcotic analgesics)
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Chemistry
Aspirin
Structure:
O
OH
O
O
Chemical name: 2-Acetyloxy benzoic acid.
Uses: To treat pain, fever and inflammation.
As a uricosuric agent and drug of choice for angina pectoris.
Adverse effect: Reye’s syndrome is characterized by acute encephalopathy (swelling of the
brain), fatty liver (swelling of the liver) mainly in children.
Formulations: Tablet and Suppository.
Brand names: Ecosprin and Disprin.
Diclofenac
Structure:
Cl
Cl
NH
OH
O
Chemical name: [2-(2,6-Dichloroanilino)phenyl]-acetic acid.
Uses: To reduce inflammation (anti-inflammatory) and as an analgesic.
Contraindication: It is contraindicated in patients with known hypersensitivity to diclofenac.
Formulations: Tablet, Injectable and Gel.
Brand names: Voveran and Diclonac.
143
Non-steroidal Anti-inflammatory Agents
Ibuprofen
Structure:
O
HO
Chemical name: (RS)-2-[4-(2-Methylpropyl)phenyl]-propanoic acid.
Uses: To reduce inflammation (anti-inflammatory) and as an analgesic.
Formulations: Tablet, Suspension and Gel.
Brand names: Brufen and Ibugesic.
Piroxicam
Structure:
N
SH
3
C
OHO
N
H
N
O O
Chemical name: 4-Hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-
carboxamide 1,1-dioxide.
Uses: It is used in the treatment of rheumatoid arthritis and osteoarthritis.
Formulations: Capsule and Injectable.
Brand names: Dolonex and Pirox.
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Chemistry
Celecoxib
Structure:
O
S
N
N
F
F
F
H
2
N
O
Chemical name:4-[5-(4-Methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]-benzenesulfonamide.
Uses: It is used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain,
musculoskeletal pain, painful menstruation.
Formulation: Tablet.
Brand names: Celcox and Cobix.
Mefenamic Acid
Structure:
NH
CH
3
H
3
C
OH
O
Chemical name: 2-(2,3-dimethylphenyl)-aminobenzoic acid.
Uses: It is used to treat moderate pain and menstrual pain.
Formulations: Tablet, Capsule and Injectable.
Brand names: Meftal and Medol.
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