Pharmacology & Therapeutics (PCG-406)

LECTURE # 03

DISCUSSION OF INDIVIDUAL ANTIHISTAMINES

CETRIZINE

Cetrizine is an anti histaminic agent (Histamine receptor antagonist). It is

classified as second generation non sedating anti histamine. Cetrizine block the

H1 receptor and produce anti-allergic effects and gives relief in allergy

symptoms such as;

 Watery eyes
 Running nose
 Sneezing
 Allergic skin disorders i-e Urticaria ( A condition where red, itchy, raised
areas of the skin occurs), Dermatitis (An inflammation of the skin that
produces a red, scaly, itchy rash is known as dermatitis).
Pharmacokinetics

Cetrizine is rapidly and extensively absorbed upon of administration in tablet or

syrup (Oral administration). Its life is 6.5 –10 hours. Cetrizine is hydrophilic

and poorly distributed in body tissues. Its metabolism takes place in liver and

excreted from the body in urine and feces.

Indications

 Dermatitis (a medical condition in which the skin becomes red, swollen

resulting irritation of the skin)

 Allergic rhinitis (Running Nose)

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 Eyes Itching (Itchy eyes can be triggered by exposure to pollen, animal

fur, mould, dust mites, make-up or eye drops. The body reacts to the

trigger by releasing histamine, causing the blood vessels in the eye to

dilate and irritating the nerve endings so the eyes water).

Contraindications

 Hypersensitivity (Hypersensitivity is abnormal sensitivity to an allergen,

drug, or other agent, where the body reacts with an exaggerated immune

response).

 Pregnancy

 Nursing mothers

Side Effects

 Sedation

 Dry mouth

 Agitation

 GI discomfort

Dosage

 Tablet 5 mg, 10mg

 Syrup 5mg/5ml

HYDROXYZINE
Hydroxyzine is a synthetic antihistaminic agent. Hydroxyzine exerts its effects

by antagonizing the effects of histamine by blocking the histaminergic receptors

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competitively/ reversibly. It is lipophilic in nature that’s why have significant

central nervous systems effects. Hydroxyzine is administered orally or

intramuscularly.

Pharmacokinetics

Hydroxyzine is rapidly absorbed from Gastro intestinal tract upon oral

administration. It is widely distributed in body tissues, metabolized in liver and

excreted in Urine.

Indications

 Anxiety

 Insomnia

 Stress

 Pruritus (severe itching of the skin)

Contraindications

 Chronic heart failure

 Glaucoma

 Constipation

 Pregnancy

Side effects

 Cardiac Arrhythmias

 Headache

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 Fatigue

 Sedation

Dosage

Tablet 10mg , 25 mg

LORATADINE

This medication is an antihistamine that treats symptoms such as itching, runny

nose, watery eyes, and sneezing and other allergies. Loratadine does not prevent

hives (Urticaria) or prevent/treat a serious allergic reaction (anaphylaxis). Hives

are raised areas of the skin that itch intensely and are red with a pale center.

Hives are a very common condition. About 20 percent of people have hives at

some time during their lives. Hives develop when there is a reaction that

activates immune cells in the skin called mast cells. When activated, these cells

release natural chemicals. One important chemical is histamine, which causes

itching, redness, and swelling of the skin in an area: a hive.

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While self-treating with this medication, it is important to read the manufacturer's

package instructions carefully. Do not use in children younger than 6 years unless

directed by the physician. Similarly, liquid or chewable tablets, should not be use

in children younger than 2 years unless directed medical practitioner. Take

Loratidine medication by mouth with or without food, usually once a day or as

directed by doctor or the product package. If chewable tablets are used, patient

should be advised to chew each tablet well and swallow. If liquid form of this

medication is used, the dose should be measured carefully.

Side Effects

A very serious allergic reaction to this drug is rare. However allergic reactions

including: rash, itching/swelling (especially of the face/tongue/throat),

severe dizziness and trouble breathing are some of the possible side effects.

CHLORPHENRAMINE

Chlorpheniramine is an antihistamine used to relieve symptoms of allergy, hay

fever, and the common cold. The symptoms include rash, watery eyes,

itchy eyes/nose/throat/skin, cough, runny nose and sneezing.

This medication works by blocking a certain natural substance (histamine and

acetylcholine) during an allergic reaction and it helps to dry up some body fluids

to relieve symptoms such as watery eyes and runny nose. Some products (such as

long-acting tablets/capsules) containing Chlorpheniramine are not recommended

for use in children younger than 12 years. These products do not cure or shorten

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the length of the common cold and may cause serious side effects. To decrease the

risk for serious side effects, carefully follow all dosage directions. Do not use this

product to make a child sleepy during cough and fever rather used only by the

directions of doctor or pharmacist and to relieve cough and cold symptoms other

measurements such as drinking enough fluids, using a humidifier or saline nose

drops/spray should be employed.

Side Effects

Drowsiness, dizziness, constipation, stomach upset, blurred vision, or dry

mouth/nose/throat may occur. To relieve dry mouth, chew (sugarless) gum, drink

water, or use a saliva substitute. If a sustained-release product is used, an empty

tablet shell may appear in stool. This is harmless.

Many people using this medication do not have serious side effects, however,

serious side effects, including: mental/mood changes (such as restlessness,

confusion), trouble urinating, fast/irregular heartbeat may occur.

Contra-Indications

It is contra-indicated or used with great cautions in the following conditions i-e

Asthma, Glaucoma, heart problems, high blood pressure, liver

disease, seizures, stomach/intestinal problems (such as ulcers,hyperthyroidism,

trouble urinating.
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This drug cause dizziness or drowsiness and blur the vision. Alcohol

or marijuana (cannabis) can enhance these effects. Do not drive, use machinery,

or do anything that needs alertness or clear vision until you can do it safely.

Drug Interactions

Some products that may interact with this drug and should be avoided to use in

combination are;

Opoids, pain or cough relievers (such as codeine, hydrocodone),

alcohol, marijuana (cannabis), drugs for sleep or anxiety (such

as alprazolam, lorazepam, zolpidem), muscle relaxants (such

as carisoprodol, cyclobenzaprine), or other antihistamines (such as cetirizine,

diphenhydramine).

Overdose

Symptoms of overdose may include: large pupils, fever, hallucinations, weakness,

shaking (tremor), muscle twitching, loss of consciousness, seizures. In children,

excitement may occur first, and may be followed by loss of coordination,

drowsiness, loss of consciousness, seizures.

MEPYRAMINE

Mepyramine belongs to first generation antihistamine targeting the

histaminergic H1 receptors. It blocks the H1 receptors reversibly/competitively

on the cell surfaces inhibiting the pathopysiological effects of histamine.

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Chemically it is an ethylenediamine derivative. It is sedating anti- histamine

and also posses’ antimuscarinic properties.

Pharmacokinetics

Mepyramine is well absorbed from GI tract after its oral administration with a

half life of 6 hours. Due to its lipophilic nature it is well distributed throughout

the body. Its metabolism takes place in liver and excreted in urine both in

metabolized and unchanged form.

Indication:

 Anxiety

 Insomnia

 Tension

 Pruritus

Contraindications

 Chronic heart diseases

 Glaucoma

 Constipation

 Pregnancy

Side Effects

 Headache

 Fatigue

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 Sedation

Dosage

 Tablet 25 mg

 Cream 20% W/W

HISTAMINE H2-RECEPTOR BLOCKERS

Histamine H2receptor (H2antagonists or H2-receptor blockers) block the

actions of histamine at all H2receptors, their chief clinical use is as inhibitors of

gastric acid secretion in the treatment of ulcers and heartburn.

FAMOTIDINE

Famotidine is used to treat ulcers of the stomach and intestines and to prevent

intestinal ulcers from coming back after they have healed. It works by decreasing

the amount of acid your stomach makes. It relieves symptoms such as cough that

doesn't go away, stomach pain, heartburn, and difficulty swallowing. Famotidine

belongs to a class of drugs known as H2 blockers. It is used to prevent and

treat heartburn and other symptoms caused by too much acid in the stomach

(acid indigestion).

It is administered orally with or without food as directed by, usually once or twice

daily right before bedtime. The dosage and length of treatment are based on

medical condition and response to therapy. In children, dosage may also be based

on body weight.

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Side Effects

Headache, constipation, or diarrhea may occur. If any of these effects persist or

worsen, tell doctor or pharmacist promptly. Many people using this medication do

not have serious side effects. Side effects, including mental/mood changes (e.g.,

restlessness, confusion, depression, hallucinations), fast/slow/irregular heartbeat,

severe dizziness, fainting, seizure.

Drug Interactions

Antifungals such as itraconazole, ketoconazole. Also do not take

this medication with other products that contain famotidine or other H2 blockers

(cimetidine, nizatidine, ranitidine).

CIMETIDINE

Cimetidine is used to treat ulcers of the stomach and intestines and prevent them

from coming back after they have healed. This medication is also used to treat

certain stomach and throat (esophagus) problems caused by too much stomach

acid. Decreasing extra stomach acid can help relieve symptoms such as stomach

pain, heartburn, difficulty swallowing, persistent cough, and trouble sleeping. It

can also prevent serious acid damage to digestive system (e.g., ulcers, cancer of

the esophagus).Cimetidine belongs to a class of drugs commonly called H2

blockers. It works by reducing the amount of acid in stomach. This medication is

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also available without a prescription. It is used to treat

occasional heartburn caused by too much acid in the stomach (also called

acid indigestion or sour stomach). It is also used to prevent heartburn and

acid indigestion caused by certain foods and beverages.

Side Effects

Mental/mood changes (e.g., agitation, confusion, depression, hallucinations),

trouble urinating, muscle/joint pain, breast swelling/soreness in males, decreased

sexual ability (with very high doses of this medication).

Drug Interactions

This medication can slow down the removal of other medications from the body,

which may affect how they work. Examples of affected drugs

include metoprolol, propranolol, warfarin, calcium channel blockers (such

as diltiazem), tricyclic antidepressants (such as amitriptyline) and theophylline.

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