Cyclizine

IUPAC nomenclature

1-benzhydryl-4-methyl-piperazine

Classification

• H1-receptor antihistamine
• Piperazine antihistamine

Physiochemical Properties

Mechanism of Action

• Cyclizine blocks the action of histamine on the receptors present at vomiting center (CTZ).
• Cyclizine also have anti-cholinergic properties, thus, it also blocks muscarinic receptors.

Structure Activity Relationship

Structure activity of piperizine antihistamines can be summarized as:

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent.
• Slow onset of action
• Low incidence of drowsiness
• They also exhibit peripheral and central antimuscarinic activity.

Method of synthesis

Alkylation of 1-methylpiperazine with benzhydrylbromide gives cyclizine. [1]

Medicinal Uses

Cyclizine is used for treatment of:

• Nausea
• Vomiting
• Dizziness
• Motion sickness

Side Effects

Side effects of cyclizine are:

• Difficult in urination
• Pounding heartbeats
• Lightheadedness
• Drowsiness
• Weakness
• Loss of coordination
• Nausea
• Dry mouth
• Constipation
• Blurred vision
• Difficult breathing
• Signs of allergic recations
• Swellings

MCQs

Q.1 Correct statements from the following related with the physicochemical properties of drug cyclizine are?

I. Molecular weight: 266.4 gm/mol

II. Appearance: White or creamy white crystalline powder

III. Melting Point: 105.5^oC

IV. Solubility: Soluble in alcohol

a) I, II, IV

b) I, III, IV

c) II, IV

d) I, II, III, IV

Q.2 Match the following of the drugs with their correct IUPAC names.

a) i-D, ii-B, iii-C, iv-A

b) i-A, ii-B, iii-D, iv-C

c) i-B, ii-C, iii-A, iv-D

d) i-A, ii-C, iii-D, iv-B

Q.3 Cyclizine has actions on?

I. Vomiting center

II. Cholinergic receptors

III. Muscarinic receptors

IV. Nicotinic receptors

a) I, III

b) I, IV

c) I, II, III

d) I

Q.4 Correct sequence for True/false for the classification of the drug can be?

• Cyclizine: H1-receptor antihistamine drug
• Haloperidol: Inhalational anesthetics
• Codeine: Narcotic analgesic
• Triclofos sodium: Sedative-hypnotics

a) TFTF

b) TTTT

c) FFTF

d) TFFT

Q.5 Piperizine antihistamine drugs are derivatives of?

a) Ethylene diamine

b) Piperidine

c) Benzodiazepine

d) Phenothiazine

Q.6 Type of rings present in the structure of cyclizine?

I. Pyridine

II. Piperazine

III. Phenyl

IV. Benzodiazepine

a) I, IV

b) I

c) II, III

d) II 

Q.7 Side effect of drug Cyclizine is/are?

a) Difficulty urination

b) Loss of coordination

c) Nausea

d) All of the above

For More Standard and Quality Question Bank you can Join Our Test Series Programme for GPAT, NIPER JEE, Pharmacist Recruitment Exam, Drug Inspector Recruitment Exams, PhD Entrance Exam for Pharmacy

Participate in Online FREE  GPAT  TEST: CLICK HERE

  Participate in Online FREE  Pharmacist  TEST: CLICK HERE 

Participate in Online FREE  Drug Inspector  TEST: CLICK HERE 

Participate in CSIR NET JRF Mock Test

Participate GATE Mock Test

ANSWERS

1-d

2-a

3-c

4-b

5-a

6-c

7-d

REFERENCES