04.drug Profile

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Department of pharmaceuticals Analysis Drug profile

DRUG PROFILE

Ketorolac

IUPAC Name: 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid

Molecular formula: C15H13NO3

Molecular weight: 255.2686

Half Life: 2.5 hours for the S-enantiomer compared with 5 hours for the R-
enantiomer

Protein binding: 99%

Category: Cyclooxygenase Inhibitors (NSAIDS)

Mechanism of action:

Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to


indomethacin and tolmetin. Ketorolac tromethamine is a racemic mixture of [-]S- and [+]R-
enantiomeric forms, with the S-form having analgesic activity. Its anti inflammatory effects
are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2
(COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased
formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The
resultant reduction in prostaglandin synthesis and activity may be at least partially
responsible for many of the adverse, as well as the therapeutic, effects of these medications.
Analgesia is probably produced via a peripheral action in which blockade of pain impulse
generation results from decreased prostaglandin activity. However, inhibition of the synthesis
or actions of other substances that sensitize pain receptors to mechanical or chemical
stimulation may also contribute to the analgesic effect. In terms of the ophthalmic
applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels
in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.

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Department of pharmaceuticals Analysis Drug profile

Structure of Ketoroloc

A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an


NSAID and is used principally for its analgesic activity. (From Martindale The Extra
Pharmacopoeia, 31st ed)

Brand Drug Drug form Manufactured Marketed Doses


Name Company Company
Cadolac Ketorolac Tablet 10mg Cadila Cadila 10mg BD
Ketlac Ketorolac Injection Neon Neon 1 ml OD
Trimethprime Laboratories
Ketiur Ketorolac Drops Sun Pharma Sun pharma 3 Drops BD
Laboratories
Ketorol Ketorolac Tablet 10mg Dr. Reddy Dr. Reddy 10mg BD
Laboratories
Nodine Ketorolac Tablet 10mg Cipla Cipla 10mg BD
Laboratories
Torolac Ketorolac Tablet 10mg Lupin Lupin 10mg BD
Laboratories
Torolac Ketorolac Injection Lupin Lupin 1ml OD
Laboratories
Torolac Ketorolac Drops Micro Micro 3 drops BD
Laboratories

Sastra college of pharmaceutical Education Page 68


Department of pharmaceuticals Analysis Drug profile

Olopatadine

IUPAC Name:

2-[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0^{3,8}]pentadeca-
1(11),3(8),4,6,12,14-hexaen-5-yl]acetic acid

Molecular formula: C21H23NO3

Molecular weight: 337.4122

Half Life: 3 hours

Category: Antihistamines

Structure:

Description

This compound belongs to the dibenzoxepines. These are compounds containing a


dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring. Used
to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine
from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo
and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine
induced effects on human conjunctival epithelial cells.

Sastra college of pharmaceutical Education Page 69


Department of pharmaceuticals Analysis Drug profile

Mechanism of action: Olopatadine is a selective histamine H1 antagonist that binds to the


histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently
leads to temporary relief of the negative symptoms brought on by histamine. Olopatadine is
devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.

Metabolism: The mono-desmethyl and the N-oxide metabolites have been detected at low
concentrations in the urine.

Route of elimination: Elimination was predominantly through renal excretion.

Brand Drug Drug form Manufactured Marketed Doses


Name Company Company
Alercher Olopatadine Eye drops Indaco indaco 3 drops BD
HCL Laboratories
If2 Olopatadine Eye drops Cipla cipla 3 drops BD
HCL Laboratories
Winolap Olopatadine Eye drops Sun sun 3 drops BD
HCL Laboratories
Allenil Olopatadine tablet Intas intas 5mg BD
HCL Laboratories
Olofast Olopatadine spray Intas intas 0.5ml BD
HCL Laboratories

Sastra college of pharmaceutical Education Page 70

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