Quality Control

ASSIGMENT

Drugs with Primary Amino group in

their structure that are given in United
States Pharmacopoeia

1. Baclofen
2. Tocainide
3. Aminocaproic acid
4. Metaraminol Bitartrate
5. Deferoxamine Mesylate

Submitted to:
Sir Shabbir Ahmed

Submitted by:
Fareeda Ibrahim DP305001
Saima Nazir DP305023
Amaara Sadia DP305039
Ayesha Baig Mirza DP305049
Maryam Shabbir DO305037

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 Primary Amino functional groups

Definition of amine:

Amines are organic compounds containing nitrogen as the key atom in the amine functional group.
Amines have structures resembling ammonia, where one or more hydrogen atoms are replaced by
alkyl groups or other groups where the nitrogen is bonded to a carbon atom in the group (groups
symbolized by R below).

However, if any of the carbons bonded to the nitrogen is part of a carbonyl group, then the compound
is considered an amide rather than an amine.

A nitrogen atom with one or two hydrogen is often referred to as an amino group.

Replacement of one, two, or all three of the hydrogen atoms in ammonia with organic groups yields
primary, secondary, or tertiary amines, respectively. Therefore, primary amino groups are those which
have two hydrogen atoms attached to nitrogen (NH2).

1. If only one the hydrogen in ammonia is replaced by a carbon based group, then it is a
primary amine.
2. If two of the hydrogen is replaced by two carbon based groups, then it is a secondary amine.
3. If all three hydrogen are replaced with three carbon based groups, then it is a tertiary amine.
4. Addition of a fourth hydrogen with an accompanying positive charge on the nitrogen atom
results in a quaternary amine.

Properties of amine:

Like ammonia, amines act as bases and are reasonably strong. The nitrogen atom has a lone electron
pair available which can accept an H+ ion to bond to the nitrogen forming a positive substituted
ammonium ion. These lone pairs also contribute to the solubility of simple amines due to hydrogen
bonding between water molecules and the lone electron pair.

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BACLOFEN

IUPAC:
Butanoic acid, 4 amino-3-(Chlorophenyl)-β-
(Aminomethyl)-p-cholorohydrocinnamic acid

Page number of USP:

1486

Class of drug:
Agaonist of the GABA receptor

Brand name:
Lioresal, Lioresal Intrathecal
Tablet: 10mg, 20mg
Intrathecal Injection: 500mcg/ml

Assay:
Baclofen was detected at 465 nm on spectrophotometer.
Reagents used:
4- Chloro- 7- Niyro- 2, 1, 3- benzoxidiazole (NBD-Cl) in non aqueous medium.
Color observed:
Orange

Solubility:
It is slight soluble in water, poorly soluble in organic solvent.
Baclofen has solubility of 750mg per 100ml in water and 2.4mg per 100ml in ethanol

Pharmacological properties
Action:
Baclofen hyperpolarizes fibers to reduce impulse transmission. It appears to reduce transmission of
impulses from spinal cord to skeletal muscles, thus decreases the frequency and amplitude of muscles
spasms in patient with spinal cord lesions

Uses:
1. Used in multiple sclerosis
2. used in spinal cord injury

Adverse effects:
Drowsiness, dizziness, headache, weakness, fatigue, insomnia, seizures, nausea, vomiting,
constipation, rash, excessive perspiration, blurred vision, slurred speech

Interaction:
Interact with CNS depressants

Contraindication:
Contraindicated in patients with hypersensitivity

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TOCAINIDE:

IUPAC:
Propanamide, 2-amino-N-(2,6-dimethylphenyl)

Page number of USP:

3424

Class of drug:
Antiarrythmic, blocks he fast Sodium Channel

Brand name:
Tonocard
Tablet: 400mg, 600mg

Assay:
Its UV detection occur at 217 nm

Solubility:
It is freely soluble in water, 1g in about 100ml alcohol, practically it is soluble in chloroform or ether.

Pharmacological properties
Action:
A class of antiarrhythmic that blocks the fast sodium channels in cardiac tissues especially the
purkinje network, without involvement of ANS. It reduces the rate of raise and amplitude of action
potential. It shortens the duration of action potential and to a lesser extent decrease the effective
refractory period.

Uses:
Used for suppression of symptomatic life threatening ventricular arrhythmias

Adverse reaction:
Ataxia, light headiness, tremor, dizziness, drowsiness, fatigue, headache, nausea, vomiting, diarrhea,
rash

Contraindicated:
It is contraindicated in patients with hypersensitivity to Lidocaine or other amide like anesthetics.

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AMINOCAPROIC ACID:

IUPAC:
Hexanoic acid, 6-amino-6-
aminohexanoic acid

Page number of USP:

1386

Class of drug:
Antifibrinolytic agent

Brand name:
Amicar
Tablet: 500mg
Syrup: 250mg/ml
Injection: 250mg/ml

Assay:
Aminocaproic acid was detected at 260 nm on spectrophotometer.
Method:
A quantitative spectrophotometric assay for aminocaproic acid and its esters based on the formation
of a chromophore upon titration with mild base has been developed.

Solubility:
It is soluble in 1g in 3ml water slightly soluble in alcohol; practically insoluble in chloroform or ether.

Pharmacological properties
Action:
Inhibit plasminogen activator substances and to a lesser degree blocks antiplasmin activity by
inhibiting fibrinolysis.

Uses:
Used in excessive bleeding resulting from hyperfibrinolysis

Adverse reactions:
Dizziness, headache, seizures, weakness, hypotension, bradycardia, arrhythmias, nausea, cramps,
diarrhea, increases ALT and AST, rash

Interaction:
Do not use with estrogen, oral contraceptives.

Contraindication:
Contraindicated in patients with hematuria , active intravascular clotting.

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METARAMINOL BITARTRATE:

IUPAC:
Benzene methanol, α-(1-aminoethyl)-3-hydroxy-2,
3-dihydroxybutanediate-α (2-aminoethyl)-m-
hydroxybenzyl alcohol tartrate

Page number of USP:

2639

Class of drug:
Adrenergic agonist

Brand name:
Aramine
Injection: 10mg/ml

Assay:
Metaraminol bitartrate was detected at 485 nm on spectrophotometer.
Reagent:
9, 10-anthraquinone-2-sulfonyl chloride

Solubility:
It is freely soluble in water, 1g in about 100ml alcohol, practically soluble in chloroform or ether

Pharmacological properties:
Action:
It stimulate alpha and beta receptors within the sympathetic nervous system causing an increase in
both systolic and diastolic blood pressure as a result of vasoconstriction

Indication:
Prevention of hypotension associated with spinal anesthesia

Adverse reaction:
Hypotension, flushing, dizziness, headache, tremors, nausea, necrosis

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DEFEROXAMINE MESYLATE:

IUPAC:
Butanediamide, N’- [5- {(4-[[5-(acetylhydroxyamino) pentyl] amino] –N- (5-
aminopentyl) –N-hydroxy -, monomthansulfonate

Page number of USP:

1885

Class of drug:

Brand name:
Desferal
Powder for injection: 500mg

Assay:
Deferoxamine mesylate was detected at 485 nm on spectrophotometer.
Assay preparation— Dissolve about 50mg of Deferoxamine Mesylate, accurately weighed, in water
to make 50.0mL, and mix
.
Pharmacological properties
Action:
Chelates ion by binding with ferric ions.

Indications or uses:
Used in adjunctive treatment of acute iron intoxication

Adverse reactions:
Tachycardia, hypotension, severe hypotension, diarrhea, urticaria, rash, fever, legs cramp

Interactions:
Don’t use with ascorbic acid it may enhance effects of deferoxamine and increases tissue toxicity of
iron.

Contraindications:
It is contraindicated in patient with severe renal disease or primary hemochromatosis

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References:

United States Pharmacopoeia

British Pharmacopoeia
Drug Nursing Guide
PharmaGuide®
Remington- The science and practice of pharmacy
Wiley InterScience Journals- Journal of Pharmaceutical Sciences
Bio-medicine.org
www.versapharm .com
www.thefreedictionary.com
www.find-health-articles.com

Brand Information taken from:

Fazal Din Pharma Plus

Fazal Din and Sons
ServAid
Zaka Pharmacy
Drug Handbook

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