بسم اهلل انرمحن انرحيم

انههم صم عهى حممد أل حممد انطيبني انطاهرين

KFU – DAMMAM

COLLEGE OF MEDCINE

207

PHARMACOLOGY – SUMMARY & REVIEW Dr. Abdulaziz Al-Khawaja

Dr. Mohammed Akram

Dr. N. B. Biswas

Done by: Ahmed Ali Al-Ghareeb

P H R M A C O L O G Y - NOTE 1 - Treatment of Asthma

أنكم اندعاءـــــنس|

2

Clin

ical

feat

ure

s o

f b

ron

chia

l as

thm

a.

•Contraction of airway smooth muscle.

•leading to acute dyspnea & airway obstruction.

•Mucus hypersecretion.•leading to mucus pulgging.

•Airway inflamation.

•leading to bronchodema.

Role of Leukotrines in asthma

Broncho-constriction

Mucosal inflammation

Mucosal edema

Mucus secretion

Drugs for Asthma

Bronchodilators

β2-adrenergic agonist

Salbutamole

Terbutaline

Salmaterol

Methylxanthines

Theophylline

Aminophylline

Anti-muscarinic

Ipratropium

Anti-inflammatory (glucorticosteroids)

Beclomethasone

Hydrocortisone

Prednisolone

Anti-leukotrienes

LT synthesis inhibitor

Zileuton

LT receptor antagonist

Montelukast

Mast cell stabilizers

Sodium Cromoglycate

Uses of bronchodilator

for acute broncho-

spasm

during acute phase of

asthma attack

for quick reduce airway

constriction

P H R M A C O L O G Y - NOTE 1 - Treatment of Asthma

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3

Bronchodilaters

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT

Β2-

adre

ner

gic

ago

nis

t

Salbutamole Fast onest.

Short duration.

Given inhaler or Nebulizer. Less side effect.

Given orally, S.C, IV or IM. Large dose. More side effect.

Bind to β-receptor & stimulate adenylcyclase.

Leading to cAMP. Bronchodilatation.

Used for acute attack. Tremor.

Vascular headache.

Terbutaline

Salmaterol Slow onest.

Long duration.

Used for long term therapy.

Met

hyl

xan

thin

es

Theophylline

Has narrow theraputic index.

Given orally.

Cause GI irritant.

Inhibit PDEI. Leading to cAMP.

Ca++

influx Bronchodilatation

1) CNS stimulation. 2) Cardiac muscle stimulation. 3) Diuresis. 4) S.M. relaxtion of bronchial & uterus. 5) Periphral & cornory vasodilatation. 6) Cerebral vasoconstriction.

GIT: nausea, vomiting .

CNS: stimulation insomnia, irritabillity & headach.

CVS: BP, arrhythmia.

Kidney: diuresis. Aminophylline

Water mixture of Theophylline + Ethylenediamine.

Given orally, rectally (suppositories) or injection.

Anti- muscrinic

Ipratropium It is poorly absobed from the GIT.

So,it given by inhalation.

Slower onest & longer duration than salbutamol.

Blocking M receptor in bronchial smooth muscle.

Bronchodilatation

Dry mouth.

Anti-inflammatory(Glucorticosteroid)

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT

Beclomethasone Given by inhalation, orally or IV. 1) Reduce mucosal edema. 2) Sensitize β2-agonist. 3) Reduce inflammatory cell activation

If taken by inhalation,

Dysphonia (hoarseness).

Oral candidiasis (fungal infection).

Hydrocortisone

Prednisolone

Anti-Leukotrienes

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT

Zileuton 1) Inhibit lipoxygenase enzyme. 2) Reduce conversion of AA to LT.

So, it is … Broncodilater. Anti-inflammatory.

To prevent asthma caused by Aspirin. NASID.

Montelukast 1) Blocking LT receptors. 2) Inhibit bronchoconstriction caused by LT

To prevent asthma caused by NASID & Exercise.

Mast Cell Stabilizers

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT

Na Cromoglycate Given by inhalation. Reduce the mediators that release from mast cell in response to allergen that cause bronchoconstriction.

Prophylaxis aginst asthma attack.

Cough.

Wheeze. Ketotifen Given orally.