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‫اﻷدوﻳﺔ ﺗﻌﻤﻞ ﻋﻠﻰ اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ‬

PHARMACOLOGY Lec11---15 Dr.Labeeb


DRUGS ACT ON RESPIRATORY SYSTEM
‫اﻟﺮﺑﻮ‬ ‫اﻟﺮﺑﻮ ﻫﻮ اﺿﻄﺮاب ﻓﻲ اﻟﻤﺠﺮى اﻟﻬﻮاﺋﻲ ﻳﺘﻤﻴﺰ ﺑﺘﻀﻴﻖ اﻟﻘﺼﺒﺎت اﻟﻬﻮاﺋﻴﺔ واﻻﻟﺘﻬﺎب‬
Asthma ، ‫ ﺗﺸﻤﻞ اﻷﻋﺮاض اﻟﻨﺎﺗﺠﺔ ﺿﻴﻖ اﻟﺘﻨﻔﺲ‬.‫وﻓﺮط اﻟﺘﻔﺎﻋﻞ ﻣﻊ اﻟﻤﺤﻔﺰات اﻟﻤﺨﺘﻠﻔﺔ‬
.. ‫ وإﻧﺘﺎج اﻟﺒﻠﻐﻢ‬، ‫ واﻟﺴﻌﺎل‬، ‫ وﺿﻴﻖ اﻟﺼﺪر‬، ‫واﻟﺼﻔﻴﺮ ﻋﻨﺪ اﻟﺘﻨﻔﺲ‬

Asthma is an airway disorder characterized by bronchoconstriction,


inflammation and hyperreactivity to various stimuli. Resultant
symptoms include dyspnea, wheezing, chest tightness, cough, and
sputum production..
Acute symptoms of asthma may be precipitated by numerous stimuli,
may initiate both inflammation and bronchoconstriction. Viral
infections of the respiratory tract are often the causative agents,
especially in infants and young children whose airways are small and
easily obstructed. Asthma symptoms may persist for days or weeks
‫ وﻗﺪ ﺗﺆدي‬، ‫ﻗﺪ ﺗﺘﺴﺒﺐ اﻷﻋﺮاض اﻟﺤﺎدة ﻟﻠﺮﺑﻮ ﻓﻲ ﺣﺪوث اﻟﻌﺪﻳﺪ ﻣﻦ اﻟﻤﺤﻔﺰات‬
after the viral infection resolves. ‫ ﻏﺎﻟ ًﺒﺎ ﻣﺎ ﺗﻜﻮن اﻻﻟﺘﻬﺎﺑﺎت‬.‫إﻟﻰ ﺣﺪوث اﻻﻟﺘﻬﺎب وﺗﻀﻴﻖ اﻟﻘﺼﺒﺎت اﻟﻬﻮاﺋﻴﺔ‬
‫ ﺧﺎﺻﺔ ﻋﻨﺪ اﻟﺮﺿﻊ واﻷﻃﻔﺎل‬، ‫اﻟﻔﻴﺮوﺳﻴﺔ ﻓﻲ اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ ﻣﻦ اﻟﻌﻮاﻣﻞ اﻟﻤﺴﺒﺒﺔ‬
‫ ﻗﺪ ﺗﺴﺘﻤﺮ‬.‫اﻟﺼﻐﺎر اﻟﺬﻳﻦ ﺗﻜﻮن ﻣﺠﺎرﻳﻬﻢ اﻟﻬﻮاﺋﻴﺔ ﺻﻐﻴﺮة وﻳﺴﻬﻞ اﻧﺴﺪادﻫﺎ‬
.‫أﻋﺮاض اﻟﺮﺑﻮ ﻷﻳﺎم أو أﺳﺎﺑﻴﻊ ﺑﻌﺪ زوال اﻟﻌﺪوى اﻟﻔﻴﺮوﺳﻴﺔ‬
In about 25% of patients with asthma, aspirin and other (NSAIDs)
can precipitate an attack. Some patients are allergic to sulfites and
may experience life-threatening asthma attacks if they ingest foods
processed with these preservatives (eg, beer, wine, dried fruit)..
‫ ﻳﻌﺎﻧﻲ ﺑﻌﺾ اﻟﻤﺮﺿﻰ ﻣﻦ‬.‫ ﻳﻤﻜﻦ أن ﻳﺆدي اﻷﺳﺒﺮﻳﻦ وﻣﻀﺎدات اﻻﻟﺘﻬﺎب ﻏﻴﺮ اﻟﺴﺘﻴﺮوﺋﻴﺪﻳﺔ اﻷﺧﺮى إﻟﻰ ﺣﺪوث ﻧﻮﺑﺔ‬، ‫ ﻣﻦ ﻣﺮﺿﻰ اﻟﺮﺑﻮ‬٪25 ‫ﻓﻲ ﺣﻮاﻟﻲ‬
.(‫ﺣﺴﺎﺳﻴﺔ ﺗﺠﺎه اﻟﻜﺒﺮﻳﺘﺎت وﻗﺪ ﻳﺘﻌﺮﺿﻮن ﻟﻨﻮﺑﺎت رﺑﻮ ﻣﻬﺪدة ﻟﻠﺤﻴﺎة إذا ﺗﻨﺎوﻟﻮا أﻃﻌﻤﺔ ﻣُ ﺠﻬﺰة ﺑﻬﺬه اﻟﻤﻮاد اﻟﺤﺎﻓﻈﺔ )ﻣﺜﻞ اﻟﺒﻴﺮة واﻟﻨﺒﻴﺬ واﻟﻔﻮاﻛﻪ اﻟﻤﺠﻔﻔﺔ‬

Gastro esophageal reflux disease (GERD), a common disorder


characterized by heartburn and esophagitis, is also associated with
asthma. Asthma that worsens at night may be associated with
nighttime acid reflux. (Asthma may also aggravate GERD, because
antiasthma medications that dilate the airways also relax muscle
tone in the gastro esophageal sphincter and may increase acid
‫ وﻫﻮ اﺿﻄﺮاب ﺷﺎﺋﻊ ﻳﺘﻤﻴﺰ ﺑﺤﺮﻗﺔ اﻟﻤﻌﺪة واﻟﺘﻬﺎب‬، (GERD) ‫ﻣﺮض اﻟﺠﺰر اﻟﻤﻌﺪي اﻟﻤﺮﻳﺌﻲ‬
reflux.) ً ‫ ﻗﺪ ﻳﺘﺮاﻓﻖ اﻟﺮﺑﻮ اﻟﺬي ﻳﺘﻔﺎﻗﻢ‬.‫أﻳﻀﺎ ﺑﺎﻟﺮﺑﻮ‬
ً ‫ ﻳﺮﺗﺒﻂ‬، ‫اﻟﻤﺮيء‬
‫ )ﻗﺪ‬.‫ﻟﻴﻼ ﻣﻊ ارﺗﺪاد اﻟﺤﻤﺾ اﻟﻠﻴﻠﻲ‬
ً ‫ﻳﺆدي اﻟﺮﺑﻮ‬
‫ ﻷن أدوﻳﺔ ﻣﻀﺎد اﻟﺮﺑﻮ اﻟﺘﻲ ﺗﻮﺳﻊ اﻟﻤﺴﺎﻟﻚ اﻟﻬﻮاﺋﻴﺔ‬، ‫أﻳﻀﺎ إﻟﻰ ﺗﻔﺎﻗﻢ ارﺗﺠﺎع اﻟﻤﺮيء‬
(.‫أﻳﻀﺎ ﻋﻠﻰ إرﺧﺎء اﻟﻌﻀﻼت ﻓﻲ اﻟﻌﻀﻠﺔ اﻟﻌﺎﺻﺮة ﻟﻠﻤﺮيء وﻗﺪ ﺗﺰﻳﺪ ﻣﻦ ارﺗﺪاد اﻟﺤﻤﺾ‬ ً ‫ﺗﻌﻤﻞ‬
I
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ اﻷدرﻳﻨﺎﻟﻴﺔ ﻓﻲ اﻟﻌﻀﻼت اﻟﻤﻠﺴﺎء ﻟﻠﻘﺼﺒﺎت‬2 ‫ ﺗﺤﻔﺰ اﻷدوﻳﺔ اﻷدرﻳﻨﺎﻟﻴﺔ ﻣﺴﺘﻘﺒﻼت ﺑﻴﺘﺎ‬:‫اﻷدرﻳﻨﺎﻟﻴﺔ‬
‫ﻣﻮﺳﻌﺎت اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ‬ ً ‫ ﺗﻌﻤﻞ ﺑﻌﺾ أدوﻳﺔ ﺑﻴﺘﺎ اﻷدرﻳﻨﺎﻟﻴﺔ‬. .‫واﻟﺸﻌﻴﺒﺎت‬
‫ اﻷدرﻳﻨﺎﻟﻴﺔ‬1 ‫أﻳﻀﺎ ﻋﻠﻰ ﺗﺤﻔﻴﺰ ﻣﺴﺘﻘﺒﻼت ﺑﻴﺘﺎ‬
Bronchodilators ‫ اﻟﺘﺤﻔﻴﺰ اﻟﻘﻠﺒﻲ ﻟﻪ ﺗﺄﺛﻴﺮ ﺿﺎر ﻋﻨﺪ إﻋﻄﺎء اﻷدوﻳﺔ ﻟﻤﻮﺳﻊ‬.‫ﻓﻲ اﻟﻘﻠﺐ ﻟﺰﻳﺎدة ﻣﻌﺪل اﻻﻧﻘﺒﺎض وﻗﻮﺗﻪ‬
.‫اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ‬
Adrenergics: Adrenergic drugs stimulate beta2-adrenergic receptors in
the smooth muscle of bronchi and bronchioles. . Some beta-adrenergic
drugs also stimulate beta1-adrenergic receptors in the heart to increase
the rate and force of contraction. Cardiac stimulation is an adverse
effect when the drugs are given for bronchodilator.
Epinephrine may be injected subcutaneously in acute attack
bronchoconstriction,. However, an inhaled selective beta2 agonist is the
‫ وﻣﻊ‬.‫اﻹﺑﻴﻨﻔﺮﻳﻦ ﻳﻤﻜﻦ ﺣﻘﻨﻪ ﺗﺤﺖ اﻟﺠﻠﺪ ﻓﻲ ﺣﺎﻟﺔ اﻟﻨﻮﺑﺔ اﻟﺤﺎدة ﺗﻀﻴﻖ اﻟﻘﺼﺒﺎت‬
drug of choice in this situation..‫ اﻻﻧﺘﻘﺎﺋﻲ ﻫﻮ اﻟﺪواء اﻟﻤﻔﻀﻞ ﻓﻲ ﻫﺬه اﻟﺤﺎﻟﺔ‬2 ‫ ﻓﺈن اﺳﺘﻨﺸﺎق ﻧﺎﻫﺾ ﺑﻴﺘﺎ‬، ‫ذﻟﻚ‬
Salbutamol (Albuterol) short-acting beta2-adrenergic agonists used
for prevention and treatment of bronchoconstriction. act more selectively
on beta2 receptors and cause less cardiac stimulation than epinephrine.
Most often taken by inhalation, they are also the most effective
bronchodilators and the treatment of first choice to relieve acute asthma.
‫ﺗﻴﺮﺑﻮﺗﺎﻟﻴﻦ ﻫﻮ ﻧﺎﻫﺾ‬
‫ اﻷدرﻳﻨﺎﻟﻲ‬2 ‫ﺑﻴﺘﺎ‬
Terbutaline is a relatively selective beta2-adrenergic agonist that is a
‫ﻧﺴﺒﻴﺎ وﻫﻮ‬
ً ‫اﻻﻧﺘﻘﺎﺋﻲ‬
‫ﻣﻮﺳﻊ ﻗﺼﺒﻲ ﻃﻮﻳﻞ‬ long-acting bronchodilator. Muscle tremor is the most frequent side
‫ رﻋﺎش‬.‫اﻟﻤﻔﻌﻮل‬
‫ اﻷدرﻳﻨﺎﻟﻴﺔ ﻗﺼﻴﺮة اﻟﻤﻔﻌﻮل ﺗﺴﺘﺨﺪم ﻟﻠﻮﻗﺎﻳﺔ‬2 ‫ﺳﺎﻟﺒﻮﺗﺎﻣﻮل )أﻟﺒﻮﺗﻴﺮول( ﻧﺎﻫﻀﺎت ﺑﻴﺘﺎ‬
‫اﻟﻌﻀﻼت ﻫﻮ اﻟﺘﺄﺛﻴﺮ‬ effect with this agent.
‫اﻟﺠﺎﻧﺒﻲ اﻷﻛﺜﺮ ﺷﻴﻮﻋً ﺎ‬ 2 ‫ ﻳﻌﻤﻞ ﺑﺸﻜﻞ أﻛﺜﺮ اﻧﺘﻘﺎﺋﻴﺔ ﻋﻠﻰ ﻣﺴﺘﻘﺒﻼت ﺑﻴﺘﺎ‬.‫واﻟﻌﻼج ﻣﻦ ﺗﻀﻴﻖ اﻟﻘﺼﺒﺎت اﻟﻬﻮاﺋﻴﺔ‬
.‫ﻟﻬﺬا اﻟﻌﺎﻣﻞ‬ ‫ وﻫﻲ‬، ‫ ﻏﺎﻟ ًﺒﺎ ﻣﺎ ﻳﺘﻢ ﺗﻨﺎوﻟﻬﺎ ﻋﻦ ﻃﺮﻳﻖ اﻻﺳﺘﻨﺸﺎق‬.‫وﻳﺴﺒﺐ ﺗﺤﻔﻴﺰ أﻗﻞ ﻟﻠﻘﻠﺐ ﻣﻦ اﻹﺑﻴﻨﻔﺮﻳﻦ‬
.‫أﻳﻀﺎ أﻛﺜﺮ ﻣﻮﺳﻌﺎت اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ ﻓﻌﺎﻟﻴﺔ وﻋﻼج اﻟﺨﻴﺎر اﻷول ﻟﺘﺨﻔﻴﻒ اﻟﺮﺑﻮ اﻟﺤﺎد‬ً
Anticholinergics
Anticholinergics block the action of acetylcholine in bronchial smooth
muscle. Ipratropium was formulated to be taken by inhalation for
maintenance therapy of bronchoconstriction associated with chronic
bronchitis and emphysema. Improved pulmonary function usually
occurs in a few minutes. Ipratropium cautious use is recommended in
patients with narrow-angle glaucoma and prostatic hypertrophy.
II ‫ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ‬
‫ ﺗﻤﺖ ﺻﻴﺎﻏﺔ‬.‫ﺗﻌﻤﻞ ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ ﻋﻠﻰ ﻣﻨﻊ ﻋﻤﻞ أﺳﺘﻴﻞ ﻛﻮﻟﻴﻦ ﻓﻲ اﻟﻌﻀﻼت اﻟﻤﻠﺴﺎء ﻟﻠﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ‬
‫اﻹﺑﺮاﺗﺮوﺑﻴﻮم ﻟﻴﺘﻢ ﺗﻨﺎوﻟﻪ ﻋﻦ ﻃﺮﻳﻖ اﻻﺳﺘﻨﺸﺎق ﻣﻦ أﺟﻞ ﻋﻼج اﻟﺼﻴﺎﻧﺔ ﻟﺘﻀﻴﻖ اﻟﻘﺼﺒﺎت اﻟﻤﺮﺗﺒﻂ ﺑﺎﻟﺘﻬﺎب اﻟﺸﻌﺐ‬
‫ ﻳﻨﺼﺢ‬.‫ ﻋﺎدة ﻣﺎ ﻳﺤﺪث ﺗﺤﺴﻦ ﻓﻲ وﻇﺎﺋﻒ اﻟﺮﺋﺔ ﻓﻲ ﻏﻀﻮن ﺑﻀﻊ دﻗﺎﺋﻖ‬.‫اﻟﻬﻮاﺋﻴﺔ اﻟﻤﺰﻣﻦ واﻧﺘﻔﺎخ اﻟﺮﺋﺔ‬
.‫ﺑﺎﺳﺘﺨﺪام إﺑﺮاﺗﺮوﺑﻴﻮم ﺑﺤﺬر ﻓﻲ اﻟﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﻌﺎﻧﻮن ﻣﻦ اﻟﺠﻠﻮﻛﻮﻣﺎ ﺿﻴﻘﺔ اﻟﺰاوﻳﺔ وﺗﻀﺨﻢ اﻟﺒﺮوﺳﺘﺎﺗﺎ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫اﻟﺰاﻧﺜﻴﻦ‬
‫ وﻳﻘﻠﻞ ﻣﻦ ﻧﻔﺎذﻳﺔ اﻷوﻋﻴﺔ‬، ‫ ﻳﻨﺘﺞ ﻟﺘﻮﺳﻴﻊ اﻟﻘﺼﺒﺎت‬.. ‫اﻟﺰاﻧﺜﻴﻦ اﻟﺮﺋﻴﺴﻲ اﻟﻤﺴﺘﺨﺪم ﺳﺮﻳﺮﻳً ﺎ ﻫﻮ اﻟﺜﻴﻮﻓﻴﻠﻴﻦ‬
ً
‫أﻳﻀﺎ ﻣﻦ اﻟﻨﺘﺎج‬ ‫ ﻳﺰﻳﺪ اﻟﺜﻴﻮﻓﻴﻠﻴﻦ‬، ‫ وﻳﺰﻳﺪ ﻣﻦ ﻗﺪرة اﻷﻫﺪاب ﻋﻠﻰ إزاﻟﺔ اﻟﻤﺨﺎط ﻣﻦ اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ‬، ‫اﻟﺪﻣﻮﻳﺔ‬
Xanthines ً
.‫ وﻳﺤﻔﺰ اﻟﺠﻬﺎز اﻟﻌﺼﺒﻲ اﻟﻤﺮﻛﺰي‬، ‫ﺧﻔﻴﻔﺎ ﻣﺪر ﻟﻠﺒﻮل‬ ‫ وﻳﻤﺎرس ﺗﺄﺛﻴﺮً ا‬، ‫ وﻳﺴﺒﺐ ﺗﻮﺳﻊ اﻷوﻋﻴﺔ اﻟﻤﺤﻴﻄﻴﺔ‬، ‫اﻟﻘﻠﺒﻲ‬

The main xanthine used clinically is theophylline.. producing to


bronchodilation, , decreasing vascular permeability, increasing the
ability of cilia to clear mucus from the airways, . Theophylline also
increases cardiac output, causes peripheral vasodilation, exerts a mild
‫اﻟﻌﻮاﻣﻞ اﻟﻤﻀﺎدة ﻟﻼﻟﺘﻬﺎﺑﺎت‬
diuretic effect, and stimulates the CNS. ‫ﺗﺴﺘﺨﺪم اﻟﻜﻮرﺗﻴﻜﻮﺳﺘﻴﺮوﻳﺪات ﻓﻲ ﻋﻼج اﻟﺮﺑﻮ اﻟﺤﺎد واﻟﻤﺰﻣﻦ واﺿﻄﺮاﺑﺎت‬
، ‫ ﻓﻠﻮﺗﻴﻜﺎﺳﻮن‬، ‫ ﻓﻠﻮﻧﻴﺴﻮﻟﻴﺪ‬، ‫ ﺑﻮدﻳﺰوﻧﻴﺪ‬، ‫ اﻟﺒﻴﻜﻠﻮﻣﻴﺜﺎزون‬، ‫اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ اﻷﺧﺮى‬
‫ ﻳﻘﻠﻞ اﻻﺳﺘﺨﺪام اﻟﻤﻮﺿﻌﻲ‬.‫وﺗﺮﻳﺎﻣﺴﻴﻨﻮﻟﻮن ﻫﻲ اﻟﻜﻮرﺗﻴﻜﻮﺳﺘﻴﺮوﻳﺪات اﻟﻤﻮﺿﻌﻴﺔ ﻟﻼﺳﺘﻨﺸﺎق‬
‫ ﻳﺘﻢ إﻋﻄﺎء اﻟﻬﻴﺪروﻛﻮرﺗﻴﺰون واﻟﺒﺮﻳﺪﻧﻴﺰون واﻟﻤﻴﺜﻴﻞ‬.‫ﻣﻦ اﻻﻣﺘﺼﺎص اﻟﺠﻬﺎزي واﻵﺛﺎر اﻟﻀﺎرة‬
‫ ﻳﺘﻢ إﻋﻄﺎء‬.‫ﺑﺮﻳﺪﻧﻴﺰوﻟﻮن ﻟﻠﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﺤﺘﺎﺟﻮن إﻟﻰ اﻟﻜﻮرﺗﻴﻜﻮﺳﺘﻴﺮوﻳﺪات اﻟﺠﻬﺎزﻳﺔ‬
Anti-inflammatory Agents ‫ ﻳﻤﻜﻦ إﻋﻄﺎء اﻟﻬﻴﺪروﻛﻮرﺗﻴﺰون واﻟﻤﻴﺜﻴﻞ ﺑﺮﻳﺪﻧﻴﺰوﻟﻮن ﻋﻦ ﻃﺮﻳﻖ‬.‫ﺑﺮﻳﺪﻧﻴﺰون ﻋﻦ ﻃﺮﻳﻖ اﻟﻔﻢ‬
.‫اﻟﻮرﻳﺪ ﻟﻠﻤﺮﺿﻰ ﻏﻴﺮ اﻟﻘﺎدرﻳﻦ ﻋﻠﻰ ﺗﻨﺎول اﻟﺪواء ﻋﻦ ﻃﺮﻳﻖ اﻟﻔﻢ‬
Corticosteroids are used in the treatment of acute and chronic asthma
and other bronchoconstrictive disorders,
Beclomethasone, budesonide, flunisolide, fluticasone, and
triamcinolone are topical corticosteroids for inhalation. Topical
administration minimizes systemic absorption and adverse effects.
Hydrocortisone, prednisone, and methylprednisolone are given to
patient who require systemic corticosteroids. Prednisone is given
orally; hydrocortisone and methylprednisolone may be given IV to
patients who are unable to take an oral medication.

Mast Cell Stabilizers


Cromolyn and nedocromil stabilize mast cells and prevent the release
of bronchoconstrictive and inflammatory substances when mast cells
are confronted with allergens and other stimuli. The drugs are indicated
only for prophylaxis of acute asthma attacks in clients with chronic
asthma.
‫ﻣﺜﺒﺘﺎت اﻟﺨﻼﻳﺎ اﻟﺒﺪﻳﻨﺔ‬
‫ﻛﺮوﻣﻮﻟﻴﻦ و ﻧﻴﺪوﻛﺮوﻣﻴﻞ ﺗﻌﻤﻞ ﻋﻠﻰ اﺳﺘﻘﺮار اﻟﺨﻼﻳﺎ اﻟﺒﺪﻳﻨﺔ وﺗﻤﻨﻊ إﻓﺮاز ﻣﻮاد‬
‫اﻟﺘﻬﺎﺑﺎت وﻣﻀﻴﻖ اﻟﺸﻌﺐ اﻟﻬﻮاﺋﻴﺔ ﻋﻨﺪﻣﺎ ﺗﻮاﺟﻪ اﻟﺨﻼﻳﺎ اﻟﺒﺪﻳﻨﺔ ﻣﺴﺒﺒﺎت‬
‫ اﻷدوﻳﺔ ﻣﻮﺻﻮﻓﺔ ﻓﻘﻂ ﻟﻠﻮﻗﺎﻳﺔ ﻣﻦ ﻧﻮﺑﺎت اﻟﺮﺑﻮ‬.‫اﻟﺤﺴﺎﺳﻴﺔ واﻟﻤﺤﻔﺰات اﻷﺧﺮى‬
III .‫اﻟﺤﺎدة ﻟﺪى اﻟﻤﺮﺿﻰ اﻟﻤﺼﺎﺑﻴﻦ ﺑﺎﻟﺮﺑﻮ اﻟﻤﺰﻣﻦ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ ﺳﺎﺑﻮﺗﺎﻣﻮل( ﻫﻮ‬، ‫ اﻷدرﻳﻨﺎﻟﻲ اﻻﻧﺘﻘﺎﺋﻲ ﻗﺼﻴﺮ اﻟﻤﻔﻌﻮل واﻟﻤﺴﺘﻨﺸﻖ )ﻋﻠﻰ ﺳﺒﻴﻞ اﻟﻤﺜﺎل‬2 ‫ ﻧﺎﻫﺾ ﺑﻴﺘﺎ‬.1
‫اﻷدوﻳﺔ اﻟﻤﻀﺎدة ﻟﻠﺮﺑﻮ‬
‫ﻋﺎدة إﻋﻄﺎء اﻷدوﻳﺔ اﻟﺘﻲ ُﺗﻌﻄﻰ ﻋﻦ ﻃﺮﻳﻖ‬
ً ‫ ﻳﻤﻜﻦ‬. .‫اﻟﺪواء اﻷول اﻟﻤﻔﻀﻞ ﻟﻠﺘﺸﻨﺞ اﻟﻘﺼﺒﻲ اﻟﺤﺎد‬
Antiasthmatic Drugs .‫اﻻﺳﺘﻨﺸﺎق ﺑﺠﺮﻋﺎت أﺻﻐﺮ وﺗﻨﺘﺞ آﺛﺎرً ا ﺿﺎﺋﺮة أﻗﻞ ﻣﻦ اﻷدوﻳﺔ اﻟﻔﻤﻮﻳﺔ أو ﺑﺎﻟﺤﻘﻦ‬

1. A selective, short-acting, inhaled beta2-adrenergic agonist (eg,


sabutamol) is the initial drug of choice for acute bronchospasm. . drugs
given by inhalation can usually be given in smaller doses and produce
fewer adverse effects than oral or parenteral drugs.
.‫ ﻣﻔﻴﺪ ﻟﻠﻐﺎﻳﺔ ﻓﻲ اﻟﺘﺪﺑﻴﺮ اﻟﻄﻮﻳﻞ اﻷﻣﺪ ﻟﻤﺮض اﻻﻧﺴﺪاد اﻟﺮﺋﻮي اﻟﻤﺰﻣﻦ‬، ‫ اﻟﻤﻮﺳﻊ اﻟﻘﺼﺒﻲ اﻟﻤﻀﺎد ﻟﻠﻜﻮﻟﻴﻦ‬، ‫ إﺑﺮاﺗﺮوﺑﻴﻮم‬.2
.‫ ﻟﻜﻨﻪ ﻳﺰﻳﺪ ﻣﻦ ﺗﺄﺛﻴﺮات ﺗﻮﺳﻴﻊ اﻟﻘﺼﺒﺎت ﻟﻸدوﻳﺔ اﻷدرﻳﻨﺎﻟﻴﺔ‬، ‫إﻧﻪ ﻏﻴﺮ ﻓﻌﺎل ﻓﻲ ﺗﺨﻔﻴﻒ اﻟﺘﺸﻨﺞ اﻟﻘﺼﺒﻲ اﻟﺤﺎد ﻓﻲ ﺣﺪ ذاﺗﻪ‬

2. Ipratropium, the anticholinergic bronchodilator, is most useful in the


long-term management of COPD. It is ineffective in relieving acute
bronchospasm by itself, but it adds to the bronchodilating effects of
adrenergic drugs.

‫ ﻳﻌﺘﺒﺮ اﻟﺜﻴﻮﻓﻴﻠﻴﻦ اﻷﻗﻞ اﺳﺘﺨﺪاﻣً ﺎ اﻵن ﻣﻦ أدوﻳﺔ اﻟﺨﻂ اﻟﺜﺎﻧﻲ‬.3

3. Theophylline less used now considered a second-line drug

.‫ ﻓﻬﻲ ﻏﻴﺮ ﻓﻌﺎﻟﺔ ﻓﻲ اﻟﺘﺸﻨﺞ اﻟﻘﺼﺒﻲ اﻟﺤﺎد‬.‫ ﻳﺴﺘﺨﺪم ﻛﺮوﻣﻮﻟﻴﻦ وﻧﻴﺪوﻛﺮوﻣﻴﻞ ﺑﺸﻜﻞ وﻗﺎﺋﻲ‬.4

4. Cromolyn and nedocromil are used prophylactically; they are


ineffective in acute bronchospasm.
‫ ﻏﺎﻟ ًﺒﺎ ﻣﺎ ﻳﺘﻢ اﺳﺘﺨﺪام‬، ‫ ﻷن اﻻﻟﺘﻬﺎب ﻗﺪ ﺛﺒﺖ أﻧﻪ ﻣﻜﻮن رﺋﻴﺴﻲ ﻟﻠﺮﺑﻮ‬.5
.‫اﻟﻜﻮرﺗﻴﻜﻮﺳﺘﻴﺮوﻳﺪ اﻟﻤﺴﺘﻨﺸﻖ ﻋﻦ ﻃﺮﻳﻖ اﻟﻔﻢ أو ﻋﻦ ﻃﺮﻳﻖ اﻟﻮرﻳﺪ ﻟﻌﺪة أﻳﺎم‬

5. Because inflammation has been established as a major component of


asthma, an inhaled corticosteroid is being used often given orally or IV
for several days.common regimen for treatment of moderate asthma

IV
‫ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb ‫آﻟﻴﺔ ﻋﻤﻞ‬
‫ﻫﻴﻜﻠﻴﺎ ﺑﺎﻟﻬﻴﺴﺘﺎﻣﻴﻦ وﺗﺤﺘﻞ ﻧﻔﺲ‬
ً ‫ﺗﺮﺗﺒﻂ ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ‬
ANTIHISTAMINES ‫ ﻣﻤﺎ ﻳﻤﻨﻊ اﻟﻬﻴﺴﺘﺎﻣﻴﻦ‬، ‫ﻣﻮاﻗﻊ اﻟﻤﺴﺘﻘﺒﻼت ﻣﺜﻞ اﻟﻬﻴﺴﺘﺎﻣﻴﻦ‬
‫ ﻓﺈن اﻷدوﻳﺔ ﻓﻌﺎﻟﺔ ﻓﻲ ﺗﺜﺒﻴﻂ ﻧﻔﺎذﻳﺔ‬، ‫ﻣﻦ اﻟﺘﺄﺛﻴﺮ ﻋﻠﻰ اﻷﻧﺴﺠﺔ اﻟﻤﺴﺘﻬﺪﻓﺔ وﺑﺎﻟﺘﺎﻟﻲ‬
Mechanism of Action ‫ واﻟﺤﻜﺔ اﻟﻤﺮﺗﺒﻄﺔ ﺑﺈﻓﺮاز‬، ‫ وﺗﻀﻴﻖ اﻟﻘﺼﺒﺎت‬، ‫ وﺗﺸﻜﻴﻞ اﻟﻮذﻣﺔ‬، ‫اﻷوﻋﻴﺔ اﻟﺪﻣﻮﻳﺔ‬
.‫ ﻓﻬﻲ ﻻ ﺗﻤﻨﻊ إﻓﺮاز اﻟﻬﻴﺴﺘﺎﻣﻴﻦ أو ﺗﻘﻠﻞ ﻣﻦ اﻟﻜﻤﻴﺔ اﻟﻤﻨﺒﻌﺜﺔ‬.‫اﻟﻬﻴﺴﺘﺎﻣﻴﻦ‬
Antihistamines are structurally related to histamine and occupy the
same receptor sites as histamine, which prevents histamine from acting
on target tissues Thus, the drugs are effective in inhibiting vascular
permeability, edema formation, bronchoconstriction, and pruritus
associated with histamine release. They do not prevent histamine
‫أﻳﻀﺎ اﻟﻌﻮاﻣﻞ ﻏﻴﺮ‬ً ‫ﻛﻴﻤﻴﺎﺋﻴﺎ )وﺗﺴﻤﻰ‬
ً ‫ﺗﺮﺗﺒﻂ ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ اﻟﻤﺘﻨﻮﻋﺔ‬
release or reduce the amount released. ‫ اﻟﻤﺮﻛﺰﻳﺔ واﻟﻤﺤﻴﻄﻴﺔ وﻳﻤﻜﻦ أن ﺗﺴﺒﺐ‬H1 ‫اﻻﻧﺘﻘﺎﺋﻴﺔ أو اﻟﻤﻬﺪﺋﺔ( ﺑﻤﺴﺘﻘﺒﻼت‬
ً
‫أﻳﻀﺎ ﺗﺄﺛﻴﺮات ﻛﺒﻴﺮة‬ ‫ﺗﺜﺒﻴﻂ اﻟﺠﻬﺎز اﻟﻌﺼﺒﻲ اﻟﻤﺮﻛﺰي )اﻟﻨﻌﺎس واﻟﺘﺨﺪﻳﺮ( وﻟﺪﻳﻬﺎ‬
‫ ﺗﺴﺒﺐ ﺟﻔﺎف اﻟﻔﻢ واﺣﺘﺒﺎس اﻟﺒﻮل‬، ‫ﻟﻤﻀﺎدات اﻟﻜﻮﻟﻴﻦ )ﻋﻠﻰ ﺳﺒﻴﻞ اﻟﻤﺜﺎل‬
H1 ‫ﻣﻀﺎدات ﻣﺴﺘﻘﺒﻼت اﻟﺠﻴﻞ اﻷول‬ ‫ ﻳﺴﺒﺐ دﻳﻜﺴﻜﻠﻮرﻓﻴﻨﻴﺮاﻣﻴﻦ )ﺑﻮﻻراﻣﻴﻦ( اﻟﺤﺪ‬.( ‫واﻹﻣﺴﺎك وﻋﺪم وﺿﻮح اﻟﺮؤﻳﺔ‬
، (‫ ﻳﺘﺴﺒﺐ دﻳﻔﻴﻨﻬﻴﺪراﻣﻴﻦ )أﻟﻴﺮﻣﻴﻦ‬.‫اﻷدﻧﻰ ﻣﻦ اﻟﻨﻌﺎس‬
First-Generation H1 Receptor Antagonists ، ‫وﻫﻮ اﻟﻨﻤﻮذج اﻷوﻟﻲ ﻟﻤﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ ﻣﻦ اﻟﺠﻴﻞ اﻷول‬
.‫ﻓﻲ ﺣﺪوث زﻳﺎدة ﻓﻲ اﻟﻨﻌﺎس وﺗﺄﺛﻴﺮات ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ‬
These chemically diverse antihistamines (also called nonselective or
sedating agents) bind to both central and peripheral H1 receptors and
can cause CNS depression (drowsiness ,sedation) They also have
substantial anticholinergic effects (eg, cause dry mouth, urinary
retention, constipation, blurred vision). Dexchlorpheniramine
(Polaramine) cause minimal drowsiness. Diphenhydramine
(Allermine), the prototype of first-generation antihistamines, causes a
high incidence of drowsiness and anticholinergic effects.

H1 ‫ﻣﻀﺎدات ﻣﺴﺘﻘﺒﻼت اﻟﺠﻴﻞ اﻟﺜﺎﻧﻲ‬

Second-Generation H1 Receptor Antagonists


Second-generation H1 antagonists (also called selective or non sedating
agents) were developed mainly to produce less sedation than the first-
generation drugs. They cause less CNS depression because they are
selective for peripheral H1 receptors and do not cross the blood–brain
barrier. Azelastine (Astelin) is the only antihistamine formulated as a
nasal spray Cetirizine . Fexofenadine.Loratadine .Desloratadine

V
ً
‫أﻳﻀﺎ اﻟﻌﻮاﻣﻞ اﻻﻧﺘﻘﺎﺋﻴﺔ أو ﻏﻴﺮ اﻟﻤﻬﺪﺋﺔ( ﺑﺸﻜﻞ أﺳﺎﺳﻲ ﻹﻧﺘﺎج ﺗﺨﺪﻳﺮ أﻗﻞ ﻣﻦ أدوﻳﺔ‬ ‫ )وﺗﺴﻤﻰ‬H1 ‫ﺗﻢ ﺗﻄﻮﻳﺮ ﻣﻀﺎدات اﻟﺠﻴﻞ اﻟﺜﺎﻧﻲ ﻣﻦ‬
ً
.‫ اﻟﻄﺮﻓﻴﺔ وﻻ ﺗﻌﺒﺮ اﻟﺤﺎﺟﺰ اﻟﺪﻣﻮي اﻟﺪﻣﺎﻏﻲ‬H1 ‫اﻧﺨﻔﺎﺿﺎ أﻗﻞ ﻓﻲ اﻟﺠﻬﺎز اﻟﻌﺼﺒﻲ اﻟﻤﺮﻛﺰي ﻷﻧﻬﺎ اﻧﺘﻘﺎﺋﻴﺔ ﻟﻤﺴﺘﻘﺒﻼت‬ ‫ إﻧﻬﺎ ﺗﺴﺒﺐ‬.‫اﻟﺠﻴﻞ اﻷول‬
‫ دﻳﺴﻠﻮراﺗﺎدﻳﻦ اﻟﺨﺎﻣﺲ‬، ‫ ﻟﻮراﺗﺎدﻳﻦ‬، ‫ ﻓﻴﻜﺴﻮﻓﻴﻨﺎدﻳﻦ‬.‫أزﻳﻼﺳﺘﻴﻦ )أﺳﺘﻠﻴﻦ( ﻫﻮ ﻣﻀﺎد اﻟﻬﻴﺴﺘﺎﻣﻴﻦ اﻟﻮﺣﻴﺪ اﻟﻤﺼﻨﻮع ﻛﺮذاذ أﻧﻔﻲ ﺳﻴﺘﺮﻳﺰﻳﻦ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ﻣﺆﺷﺮات ﻟﻼﺳﺘﺨﺪام‬
‫ﺗﺴﺘﺨﺪم ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ ﻟﻤﺠﻤﻮﻋﺔ ﻣﺘﻨﻮﻋﺔ ﻣﻦ اﺿﻄﺮاﺑﺎت‬
‫اﻟﺤﺴﺎﺳﻴﺔ وﻏﻴﺮ اﻟﺘﺤﺴﺴﻴﺔ‬
Indications for Use ‫اﻟﺘﻬﺎب اﻷﻧﻒ اﻟﺘﺤﺴﺴﻲ‬
.. ‫• اﻟﺤﺴﺎﺳﻴﺔ اﻟﻤﻔﺮﻃﺔ‬
Antihistamines are used for a variety of allergic and .‫• اﻟﺘﻬﺎب اﻟﻤﻠﺘﺤﻤﺔ اﻟﺘﺤﺴﺴﻲ‬
.‫• اﻟﺤﺴﺎﺳﻴﺔ اﻟﺪواﺋﻴﺔ واﻟﺤﺴﺎﺳﻴﺔ اﻟﺰاﺋﻔﺔ‬
.‫• ﻋﻤﻠﻴﺎت ﻧﻘﻞ اﻟﺪم وﻣﺸﺘﻘﺎﺗﻪ‬
nonallergicdisorders .. ‫• اﻷﻣﺮاض اﻟﺠﻠﺪﻳﺔ‬

Allergic rhinitis ‫ ُﺗﺴﺘﺨﺪم ﺑﻌﺾ ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ ﺑﺸﻜﻞ ﺷﺎﺋﻊ‬.‫• ﻣﺘﻨﻮع‬


‫ ﻣﺜﻞ دوار اﻟﺤﺮﻛﺔ واﻟﻐﺜﻴﺎن‬، ‫ﻟﻼﺿﻄﺮاﺑﺎت ﻏﻴﺮ اﻟﺘﺤﺴﺴﻴﺔ‬
• Anaphylaxis.. ‫ ﻫﻴﺪروﻛﺴﻴﺰﻳﻦ ؛‬، ‫ ﺑﺮوﻣﻴﺜﺎزﻳﻦ‬، ‫واﻟﻘﻲء )ﻋﻠﻰ ﺳﺒﻴﻞ اﻟﻤﺜﺎل‬
‫ اﻟﻌﻨﺼﺮ‬.(‫ دﻳﻔﻴﻨﻬﻴﺪراﻣﻴﻦ‬، ‫واﻟﻨﻮم )ﻋﻠﻰ ﺳﺒﻴﻞ اﻟﻤﺜﺎل‬
• Allergic conjunctivitis. ‫اﻟﻨﺸﻂ ﻓﻲ ﻣﺴﺎﻋﺪات اﻟﻨﻮم اﻟﻤﺘﺎﺣﺔ ﺑﺪون وﺻﻔﺔ ﻃﺒﻴﺔ ﻫﻮ‬
.‫ﻣﻀﺎد ﻟﻠﻬﺴﺘﺎﻣﻴﻦ‬

• Drug allergies and pseudoallergies.


• Transfusions of blood and blood products.
• Dermatologic conditions..

• Miscellaneous. Some antihistamines are commonly used for


nonallergic disorders, such as motion sickness, nausea and vomiting
(eg, promethazine, hydroxyzine; and sleep (eg, diphenhydramine). The
active ingredient in OTC sleep aids is a sedating antihistamine.

Contraindications to Use
Antihistamines are contraindicated or must be used with caution in
clients with hypersensitivity to the drugs, narrow angle glaucoma,
prostatic hypertrophy, and bladder neck obstruction, and during
pregnancy
‫ﻣﻮاﻧﻊ ﻟﻼﺳﺘﺨﺪام‬
‫ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ ﻣﻤﻨﻮﻋﺔ أو ﻳﺠﺐ اﺳﺘﺨﺪاﻣﻬﺎ ﺑﺤﺬر ﻓﻲ‬
‫ واﻟﺰرق ﺿﻴﻖ‬، ‫اﻟﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﻌﺎﻧﻮن ﻣﻦ ﻓﺮط اﻟﺤﺴﺎﺳﻴﺔ ﻟﻸدوﻳﺔ‬
.‫ وأﺛﻨﺎء اﻟﺤﻤﻞ‬، ‫ واﻧﺴﺪاد ﻋﻨﻖ اﻟﻤﺜﺎﻧﺔ‬، ‫ وﺗﻀﺨﻢ اﻟﺒﺮوﺳﺘﺎت‬، ‫اﻟﺰاوﻳﺔ‬

VI
‫ﺳﻌﺎل‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ ﻋﺎدة ﻣﺎ ﻳﻜﻮن رد ﻓﻌﻞ وﻗﺎﺋﻲ ﻹزاﻟﺔ‬.‫• اﻟﺴﻌﺎل ﻫﻮ ﻃﺮد ﻗﻮي ﻟﻠﻬﻮاء ﻣﻦ اﻟﺮﺋﺘﻴﻦ‬
Cough .‫اﻷﺟﺴﺎم اﻟﻐﺮﻳﺒﺔ أو اﻟﻤﻬﻴﺠﺎت اﻟﺒﻴﺌﻴﺔ أو اﻹﻓﺮازات اﻟﻤﺘﺮاﻛﻤﺔ ﻣﻦ اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ‬
.‫ﻳﺸﻤﻞ رد ﻓﻌﻞ اﻟﺴﻌﺎل آﻟﻴﺎت ﻣﺮﻛﺰﻳﺔ وﻃﺮﻓﻴﺔ‬

• Cough is a forceful expulsion of air from the lungs. It is normally a


protective reflex for removing foreign bodies, environmental irritants,
or accumulated secretions from the respiratory tract.
The cough reflex involves central and peripheral mechanisms.
‫ ﻳﺘﻠﻘﻰ ﻣﺮﻛﺰ‬، ‫ﻣﺮﻛﺰﻳً ﺎ‬
‫اﻟﺴﻌﺎل ﻓﻲ اﻟﻨﺨﺎع‬
Centrally, the cough center in the medulla oblongata receives stimuli
‫اﻟﻤﺴﺘﻄﻴﻞ اﻟﻤﻨﺒﻬﺎت‬
‫وﻳﺒﺪأ اﻻﺳﺘﺠﺎﺑﺔ‬ and initiates the reflex response
، ‫اﻻﻧﻌﻜﺎﺳﻴﺔ اﻟﻤﺤﻴﻄﻴﺔ‬
‫وﻣﺴﺘﻘﺒﻼت اﻟﺴﻌﺎل ﻓﻲ‬ Peripherally, cough receptors in the pharynx, larynx, trachea, or lungs
‫اﻟﺒﻠﻌﻮم أو اﻟﺤﻨﺠﺮة أو‬
‫اﻟﻘﺼﺒﺔ اﻟﻬﻮاﺋﻴﺔ أو‬ may be stimulated by air, dryness of mucous membranes, or excessive
‫اﻟﺮﺋﺘﻴﻦ‬
‫ﻳﻤﻜﻦ ﺗﺤﻔﻴﺰﻫﺎ ﺑﺎﻟﻬﻮاء‬
‫أو ﺟﻔﺎف اﻷﻏﺸﻴﺔ‬
secretions.
‫اﻟﻤﺨﺎﻃﻴﺔ أو اﻹﻓﺮازات‬
.‫اﻟﺰاﺋﺪة‬ There are two type of cough: the useful and the useless.
Cough is useful when it effectively expels secretions or foreign material
from the respiratory tract, i.e. when it is productive; it is useless when it is
unproductive and persistent.
Useful cough should be allowed to serve its purpose and suppressed only
when it is exhausting the patient or is dangerous ,e.g. after surgery. Useless
.‫ اﻟﻤﻔﻴﺪ وﻏﻴﺮ اﻟﻨﺎﻓﻊ‬:‫ﻫﻨﺎك ﻧﻮﻋﺎن ﻣﻦ اﻟﺴﻌﺎل‬
persistent cough should be stopped.. ‫ﻳﻜﻮن اﻟﺴﻌﺎل ﻣﻔﻴﺪً ا ﻋﻨﺪﻣﺎ ﻳﻄﺮد ﺑﺸﻜﻞ ﻓﻌﺎل اﻹﻓﺮازات أو اﻟﻤﻮاد اﻟﻐﺮﻳﺒﺔ‬
‫ﻣﻨﺘﺠﺎ ؛ ﻻ ﺟﺪوى ﻣﻨﻬﺎ ﻋﻨﺪﻣﺎ ﺗﻜﻮن‬
ً ‫ أي ﻋﻨﺪﻣﺎ ﻳﻜﻮن‬، ‫ﻣﻦ اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ‬
‫ ﻳﺠﺐ اﻟﺴﻤﺎح ﻟﻠﺴﻌﺎل اﻟﻤﻔﻴﺪ أن ﻳﺨﺪم اﻟﻐﺮض ﻣﻨﻪ‬.‫ﻏﻴﺮ ﻣﻨﺘﺠﺔ وﻣﺴﺘﻤﺮة‬
ً
‫ ﻋﻠﻰ ﺳﺒﻴﻞ‬، ‫ﻣﺮﻫﻘﺎ ﻟﻠﻤﺮﻳﺾ أو ﻳﻜﻮن ﺧﻄﻴﺮً ا‬ ‫وﻗﻤﻌﻪ ﻓﻘﻂ ﻋﻨﺪﻣﺎ ﻳﻜﻮن‬
COUGH SUPPRESSION .. ‫ ﻳﺠﺐ إﻳﻘﺎف اﻟﺴﻌﺎل اﻟﻤﺴﺘﻤﺮ ﻋﺪﻳﻢ اﻟﻔﺎﺋﺪة‬.‫ ﺑﻌﺪ اﻟﺠﺮاﺣﻪ‬.‫اﻟﻤﺜﺎل‬

Antitussives that act centrally


The most consistent means of suppressing cough is blockade of the
medullary cough centre itself. Opioids, such as codeine, are very effective
antitussive ..There are also nonopioid antitussive dextromethorphan . have
no significant analgesic or respiratory depressant effects at the doses
required for their antitussive action .
‫ﻗﻤﻊ اﻟﺴﻌﺎل‬
‫ﻣﻀﺎدات اﻟﺴﻌﺎل اﻟﺘﻲ ﺗﻌﻤﻞ ﺑﺸﻜﻞ ﻣﺮﻛﺰي‬
.‫اﺗﺴﺎﻗﺎ ﻫﻲ ﺣﺼﺎر ﻣﺮﻛﺰ اﻟﺴﻌﺎل اﻟﻨﺨﺎﻋﻲ ﻧﻔﺴﻪ‬ً ‫أﻛﺜﺮ وﺳﺎﺋﻞ ﻗﻤﻊ اﻟﺴﻌﺎل‬
.. ‫ ﻓﻌﺎﻟﺔ ﺟﺪً ا ﻓﻲ ﻋﻼج اﻟﺴﻌﺎل‬، ‫ ﻣﺜﻞ اﻟﻜﻮداﻳﻴﻦ‬، ‫اﻟﻤﻮاد اﻷﻓﻴﻮﻧﻴﺔ‬
VII ‫ ﻟﻴﺲ ﻟﻬﺎ‬.‫أﻳﻀﺎ دﻳﻜﺴﺘﺮوﻣﻴﺜﻮرﻓﺎن ﻣﻀﺎد ﻟﻠﺴﻌﺎل ﻏﻴﺮ أﻓﻴﻮﻧﻲ‬ ً ‫وﻫﻨﺎك‬
‫ﺗﺄﺛﻴﺮات ﻣﺴﻜﻨﺔ أو ﻣﺜﺒﻄﺔ ﻟﻠﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ ﻋﻨﺪ اﻟﺠﺮﻋﺎت اﻟﻤﻄﻠﻮﺑﺔ‬
.‫ﻟﺘﺄﺛﻴﺮﻫﺎ اﻟﻤﻀﺎد ﻟﻠﺴﻌﺎل‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ﻣﺤﻠﻴﺎ )ﻣﺜﻞ ﻣﺴﺘﺤﻠﺒﺎت اﻟﺤﻠﻖ وﻗﻄﺮات اﻟﺴﻌﺎل( ﻗﺪ ﺗﻤﻨﻊ اﻟﺴﻌﺎل ﻋﻦ ﻃﺮﻳﻖ زﻳﺎدة ﺗﺪﻓﻖ اﻟﻠﻌﺎب واﺣﺘﻮاء اﻟﻤﻮاد‬ ً ‫اﻟﻌﻮاﻣﻞ اﻟﻤﺆﺛﺮة‬
.‫ ﻏﺎﻟ ًﺒﺎ ﻣﺎ ﺗﺴﺘﺨﺪم اﻟﻌﺼﺎﺋﺮ اﻟﻤﻨﻜﻬﺔ ﻛﻮﺳﻴﻠﺔ ﻟﻌﻘﺎﻗﻴﺮ أﺧﺮى‬.‫اﻟﻤﻠﻄﻔﺔ أو اﻟﺘﺨﺪﻳﺮ اﻟﻤﻮﺿﻌﻲ ﻟﺘﻘﻠﻴﻞ ﺗﻬﻴﺞ اﻟﻐﺸﺎء اﻟﻤﺨﺎﻃﻲ ﻟﻠﺒﻠﻌﻮم‬
Locally acting agents (eg, throat lozenges, cough drops) may suppress
cough by increasing the flow of saliva and by containing demulcents or
local anesthetics to decrease irritation of pharyngeal mucosa. Flavored
‫ﻳﺘﻤﺜﻞ اﻟﻤﺆﺷﺮ اﻟﺴﺮﻳﺮي اﻟﺮﺋﻴﺴﻲ ﻟﻤﻀﺎدات اﻟﺴﻌﺎل ﻓﻲ‬
syrups are often used as vehicles for other drugs. .‫اﻟﺴﻌﺎل اﻟﺠﺎف ﻏﻴﺮ اﻟﻤﻨﺘﺞ اﻟﺬي ﻳﺘﺪاﺧﻞ ﻣﻊ اﻟﺮاﺣﺔ واﻟﻨﻮم‬
‫ﻟﻴﺲ ﻣﻦ اﻟﻤﺴﺘﺤﺴﻦ ﻗﻤﻊ اﻟﺴﻌﺎل اﻟﻤﻨﺘﺞ ﻷن اﻹﻓﺮازات‬
The major clinical indication of antitussives is a dry , , nonproductive .‫ﺗﺤﺘﺎج إﻟﻰ إزاﻟﺘﻬﺎ‬

cough that interferes with rest and sleep. It is not desirable to suppress a
‫ﻣﻘﺸﻊ‬
productive cough because the secretions need to be removed. ‫اﻟﻤﻮاد اﻟﻄﺎردة ﻟﻠﺒﻠﻐﻢ ﻫﻲ ﻋﻮاﻣﻞ‬
‫ُﺗﻌﻄﻰ ﻋﻦ ﻃﺮﻳﻖ اﻟﻔﻢ ﻟﺘﺴﻴﻴﻞ إﻓﺮازات اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ واﻟﺴﻤﺎح ﺑﺈزاﻟﺘﻬﺎ‬
*Guaifenesin Expectorants ‫ )ﺟﻠﻴﺴﺮﻳﻞ ﺟﻮاﻳﺎﻛﻮﻻﺗﻲ( أﻛﺜﺮ ﻣﻘﺸﻊ‬Guaifenesin ‫ ﻳﻌﺪ‬.‫ﺑﺴﻬﻮﻟﺔ‬
‫ﻣﻘﺸﻊ ﻳﺴﺘﺨﺪم ﻓﻲ‬ ‫ ﻳﺘﻮﻓﺮ ﺑﻤﻔﺮده وﻛﻤﻜﻮن ﻓﻲ اﻟﻌﺪﻳﺪ ﻣﻦ ﻋﻼﺟﺎت‬.‫ﻟﻠﺒﻠﻐﻢ اﺳﺘﺨﺪاﻣً ﺎ‬
‫ﺷﺮاب اﻟﺴﻌﺎل‬ ، ‫اﻟﺴﻌﺎل واﻟﺒﺮد‬
ً
‫وأﺣﻴﺎﻧﺎ ﻟﺘﺨﻔﻴﻒ‬
Expectorants are agents given orally to liquefy respiratory secretions
‫اﻵﻻم ﻣﻦ اﻷﻟﻢ‬
.‫اﻟﻌﻀﻠﻲ اﻟﻠﻴﻔﻲ‬ and allow for their easier removal. Guaifenesin (glyceryl guaiacolate )is
the most commonly used expectorant. It is available alone and as an
ingredient in many combination cough and cold remedies,
‫ﻣﻴﻮﻛﻮﻟﻴﺘﻴﻚ‬
Mucolytics ‫ وﻳﻜﻮن‬، ‫ُﺗﻌﻄﻰ أدوﻳﺔ ﺣﺎل ﻟﻠﺒﻠﻐﻢ ﻟﺘﺴﻴﻴﻞ اﻟﻤﺨﺎط ﻓﻲ اﻟﺠﻬﺎز اﻟﺘﻨﻔﺴﻲ‬
.‫اﻷﺳﻴﺘﻴﻞ ﺳﻴﺴﺘﺌﻴﻦ ﻓﻌﺎﻻً ﻓﻲ ﻏﻀﻮن دﻗﻴﻘﺔ واﺣﺪة ﺑﻌﺪ اﻻﺳﺘﻨﺸﺎق‬
Mucolytics are administered to liquefy mucus in the respiratory
tract.Acetylcysteine is effective within 1 minute after inhalation. ‫ﻋﻼﺟﺎت اﻟﺒﺮد‬
‫ﺗﺘﻮﻓﺮ اﻟﻌﺪﻳﺪ ﻣﻦ اﻟﻤﻨﺘﺠﺎت اﻟﻤﺮﻛﺒﺔ ﻟﻌﻼج أﻋﺮاض‬
Cold Remedies ‫ ﺗﺤﺘﻮي اﻟﻌﺪﻳﺪ ﻣﻦ اﻟﻤﻨﺘﺠﺎت ﻋﻠﻰ‬.‫ﻧﺰﻻت اﻟﺒﺮد‬
.‫ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ وﻣﺰﻳﻞ اﺣﺘﻘﺎن اﻷﻧﻒ وﻣﺴﻜﻦ‬
Many combination products are available for treating symptoms of the
common cold. Many of the products contain an antihistamine, a nasal
decongestant, and an analgesic. Some contain antitussives,
expectorants, and other agents as well. Many cold remedies are over-
the-counter (OTC) formulations. Commonly used ingredients include
chlorpheniramine (antihistamine), pseudoephedrine (adrenergic nasal
decongestant), acetaminophen (analgesic and antipyretic),
dextromethorphan (antitussive), and guaifenesin (expectorant).
ً
‫ اﻟﻌﺪﻳﺪ ﻣﻦ‬.‫أﻳﻀﺎ‬ ‫ﻳﺤﺘﻮي ﺑﻌﻀﻬﺎ ﻋﻠﻰ ﻣﻀﺎدات اﻟﺴﻌﺎل واﻟﺒﻠﻐﻢ وﻋﻮاﻣﻞ أﺧﺮى‬
‫ ﺗﺸﻤﻞ اﻟﻤﻜﻮﻧﺎت‬.(OTC) ‫ﻋﻼﺟﺎت اﻟﺒﺮد ﻫﻲ ﺗﺮﻛﻴﺒﺎت ﺑﺪون وﺻﻔﺔ ﻃﺒﻴﺔ‬
‫اﻟﻤﺴﺘﺨﺪﻣﺔ ﺑﺸﻜﻞ ﺷﺎﺋﻊ ﻛﻠﻮرﻓﻴﻨﻴﺮاﻣﻴﻦ )ﻣﻀﺎدات اﻟﻬﻴﺴﺘﺎﻣﻴﻦ( وﺳﻮدوإﻳﻔﻴﺪرﻳﻦ‬
VIII (‫)ﻣﺰﻳﻞ اﺣﺘﻘﺎن اﻷﻧﻒ اﻷدرﻳﻨﺎﻟﻲ( وأﺳﻴﺘﺎﻣﻴﻨﻮﻓﻴﻦ )ﻣﺴﻜﻦ وﺧﺎﻓﺾ ﻟﻠﺤﺮارة‬
.(‫ودﻳﻜﺴﺘﺮوﻣﻴﺜﻮرﻓﺎن )ﻣﻀﺎد ﻟﻠﺴﻌﺎل( وﺟﻮاﻳﻔﻴﻨﻴﺴﻴﻦ )ﻣﻘﺸﻊ‬
‫ﻣﻀﺎدات اﻟﺤﻤﻮﺿﺔ‬
‫ﻗﻮاﻋﺪ ﺿﻌﻴﻔﺔ ﺗﺘﻔﺎﻋﻞ ﻣﻊ ﺣﻤﺾ اﻟﻬﻴﺪروﻛﻠﻮرﻳﻚ اﻟﻤﻌﺪي ﻟﺘﻜﻮﻳﻦ ﻣﻠﺢ‬
‫ادوﻳﺔ ﺗﻌﻤﻞ ﻋﻠﻰ اﻟﺠﻬﺎز اﻟﻬﻀﻤﻲ‬ ‫ ﺳﺎﻋﺔ‬/ ‫ ﻣﻠﻲ ﻣﻜﺎﻓﺊ‬45 ‫ ﻳﺘﻢ إﻓﺮاز ﻣﺎ ﻳﻘﺮب ﻣﻦ‬، ‫ ﺑﻌﺪ اﻟﻮﺟﺒﺔ‬.‫وﻣﺎء‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ ﻣﻴﻜﺮوﻟﺘﺮ ﻣﻦ‬156 ‫ ﺟﺮﻋﺔ واﺣﺪة ﻣﻦ‬.‫ﻣﻦ ﺣﻤﺾ اﻟﻬﻴﺪروﻛﻠﻮرﻳﻚ‬
Drugs act on GIT ‫ﻣﻀﺎد اﻟﺤﻤﻮﺿﺔ ﺗﻌﻄﻰ ﺑﻌﺪ ﺳﺎﻋﺔ واﺣﺪة ﻣﻦ اﻟﻮﺟﺒﺔ ﺗﺤﻴﺪ ﺑﺸﻜﻞ‬
‫ وﻗﺪ اﺳﺘﺨﺪﻣﺖ ﻓﻲ‬، ‫ﻓﻌﺎل ﺣﻤﺾ اﻟﻤﻌﺪة ﻟﻤﺪة ﺗﺼﻞ إﻟﻰ ﺳﺎﻋﺘﻴﻦ‬
ANTACIDS ‫ ﻣﻊ اﻟﺤﻤﻮﺿﺔ اﻟﻤﻌﻮﻳﺔ اﻟﻤﺘﻘﻄﻌﺔ وﻋﺴﺮ اﻟﻬﻀﻢ‬.‫ﻋﻼج اﻟﻤﺮﺿﻰ‬
.‫واﺿﻄﺮاﺑﺎت اﻟﻬﻀﻢ اﻟﺤﻤﻀﻴﺔ‬

weak bases that react with gastric HCL to form a salt and water. After
meal, approximately 45 mEq/h of HCL secreted. A single dose of 156
mEq of antacid given 1 hour after a meal effectively neutralizes gastric
acid for up to 2 hours, have been used in the treatment of patients. With
intermittent heartburn and dyspepsia and acid-peptic disorders .
Sodium bicarbonate reacts rapidly with HCl to produce carbon
dioxide and NaCl, Sodium chloride absorption may exacerbate fluid
retention in patients with heart failure, hypertension, and renal
‫ﺑﻴﻜﺮﺑﻮﻧﺎت اﻟﺼﻮدﻳﻮم ﺗﺘﻔﺎﻋﻞ ﺑﺴﺮﻋﺔ ﻣﻊ ﺣﻤﺾ اﻟﻬﻴﺪروﻛﻠﻮرﻳﻚ ﻹﻧﺘﺎج اﻟﻜﺮﺑﻮن‬
insufficiency. ‫ﻗﺪ ﻳﺆدي اﻣﺘﺼﺎص ﻛﻠﻮرﻳﺪ اﻟﺼﻮدﻳﻮم وﺛﺎﻧﻲ أﻛﺴﻴﺪ اﻟﺼﻮدﻳﻮم وﻛﻠﻮرﻳﺪ اﻟﺼﻮدﻳﻮم إﻟﻰ ﺗﻔﺎﻗﻢ‬
.‫اﺣﺘﺒﺎس اﻟﺴﻮاﺋﻞ ﻓﻲ اﻟﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﻌﺎﻧﻮن ﻣﻦ ﻗﺼﻮر اﻟﻘﻠﺐ وارﺗﻔﺎع ﺿﻐﻂ اﻟﺪم واﻟﻘﺼﻮر اﻟﻜﻠﻮي‬

Calcium carbonate is less soluble and reacts more slowly than sodium
bicarbonate with HCl to form carbon dioxide and CaCl2. Excessive
doses calcium carbonate with calcium-containing dairy products can
lead to hypercalcemia, renal insufficiency, and metabolic alkalosis
‫ﻛﺮﺑﻮﻧﺎت اﻟﻜﺎﻟﺴﻴﻮم أﻗﻞ ﻗﺎﺑﻠﻴﺔ ﻟﻠﺬوﺑﺎن وﺗﺘﻔﺎﻋﻞ ﺑﺸﻜﻞ أﺑﻄﺄ ﻣﻦ ﺑﻴﻜﺮﺑﻮﻧﺎت اﻟﺼﻮدﻳﻮم ﻣﻊ ﺣﻤﺾ اﻟﻬﻴﺪروﻛﻠﻮرﻳﻚ‬
(milk-alkali syndrome). ‫ اﻟﺠﺮﻋﺎت اﻟﺰاﺋﺪة ﻣﻦ ﻛﺮﺑﻮﻧﺎت اﻟﻜﺎﻟﺴﻴﻮم ﻣﻊ ﻣﻨﺘﺠﺎت اﻷﻟﺒﺎن اﻟﻤﺤﺘﻮﻳﺔ‬.CaCl2 ‫ﻟﺘﻜﻮﻳﻦ ﺛﺎﻧﻲ أﻛﺴﻴﺪ اﻟﻜﺮﺑﻮن و‬
.(‫ ﻗﻼء اﺳﺘﻘﻼﺑﻲ )ﻣﺘﻼزﻣﺔ اﻟﺤﻠﻴﺐ اﻟﻘﻠﻮي‬، ‫ ﻗﺼﻮر ﻛﻠﻮي‬، ‫ﻋﻠﻰ اﻟﻜﺎﻟﺴﻴﻮم ﻳﻤﻜﻦ أن ﺗﺆدي إﻟﻰ ﻓﺮط ﻛﺎﻟﺴﻴﻮم اﻟﺪم‬

Formulations(magnesium hydroxide or aluminum hydroxide) react


slowly with HCl to form magnesium chloride or aluminum chloride
and water. no gas is generated,. Because unabsorbed magnesium salts
may cause an osmotic diarrhea and aluminum salts may cause
constipation, these agents are commonly administered together in
proprietary formulations (eg, Gelusil, Maalox) to minimize the impact
upon bowel function. Both magnesium and aluminum are absorbed and
excreted by the kidneys. Hence, patients with renal insufficiency
should not take these agents long-term.
(‫ﺗﺘﻔﺎﻋﻞ اﻟﺘﺮﻛﻴﺒﺎت )ﻫﻴﺪروﻛﺴﻴﺪ اﻟﻤﻐﻨﻴﺴﻴﻮم أو ﻫﻴﺪروﻛﺴﻴﺪ اﻷﻟﻮﻣﻨﻴﻮم‬
‫ﺑﺒﻂء ﻣﻊ ﺣﻤﺾ اﻟﻬﻴﺪروﻛﻠﻮرﻳﻚ ﻟﺘﻜﻮﻳﻦ ﻛﻠﻮرﻳﺪ اﻟﻤﻐﻨﻴﺴﻴﻮم أو ﻛﻠﻮرﻳﺪ‬
‫ ﻧﻈﺮً ا ﻷن أﻣﻼح اﻟﻤﻐﻨﻴﺴﻴﻮم ﻏﻴﺮ‬.‫ ﻻ ﻳﻮﺟﺪ ﻏﺎز ﻣﺘﻮﻟﺪ‬.‫اﻷﻟﻮﻣﻨﻴﻮم واﻟﻤﺎء‬
‫ﺗﻨﺎﺿﺤﻴﺎ وﻗﺪ ﺗﺴﺒﺐ أﻣﻼح اﻷﻟﻮﻣﻨﻴﻮم‬
ً ً
‫إﺳﻬﺎﻻ‬ ‫اﻟﻤﻤﺘﺼﺔ ﻗﺪ ﺗﺴﺒﺐ‬
IX ً
‫ﻋﺎدة ﻣﻌً ﺎ ﻓﻲ ﺗﺮﻛﻴﺒﺎت ﺧﺎﺻﺔ )ﻣﺜﻞ‬ ‫ ﻓﺈن ﻫﺬه اﻟﻌﻮاﻣﻞ ُﺗﻌﻄﻰ‬، ‫إﻣﺴﺎﻛًﺎ‬
‫ ﻳﺘﻢ‬.‫ و ﻣﺎﻟﻮﻛﺲ( ﻟﺘﻘﻠﻴﻞ اﻟﺘﺄﺛﻴﺮ ﻋﻠﻰ وﻇﻴﻔﺔ اﻷﻣﻌﺎء‬، ‫ﺟﻴﻠﻮﺳﻴﻞ‬
.‫اﻣﺘﺼﺎص ﻛﻞ ﻣﻦ اﻟﻤﻐﻨﻴﺴﻴﻮم واﻷﻟﻤﻨﻴﻮم وإﻓﺮازﻫﻤﺎ ﻋﻦ ﻃﺮﻳﻖ اﻟﻜﻠﻰ‬
‫ ﻳﺠﺐ ﻋﻠﻰ ﻣﺮﺿﻰ اﻟﻘﺼﻮر اﻟﻜﻠﻮي ﻋﺪم ﺗﻨﺎول ﻫﺬه اﻷدوﻳﺔ ﻋﻠﻰ‬، ‫وﻣﻦ ﺛﻢ‬
.‫اﻟﻤﺪى اﻟﻄﻮﻳﻞ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb

Drugs Used In Acid-Peptic Diseases


Acid-peptic diseases include gastro esophageal reflux, peptic ulcer
(gastric and duodenal), and stress-related mucosal injury. In all these
conditions, mucosal erosions or ulceration arise when the caustic
effects of aggressive factors (acid, pepsin, bile) overwhelm the
defensive factors of the gastrointestinal mucosa (mucus and
bicarbonate secretion, prostaglandins, blood flow, and the processes of
‫اﻷدوﻳﺔ اﻟﻤﺴﺘﺨﺪﻣﺔ ﻓﻲ اﻷﻣﺮاض اﻟﺤﻤﻀﻴﺔ اﻟﻬﻀﻤﻴﺔ‬
restitution and regeneration after cellular injury). ‫ﺗﺸﻤﻞ اﻷﻣﺮاض اﻟﻤﻌﻮﻳﺔ اﻟﺤﻤﻀﻴﺔ ارﺗﺠﺎع اﻟﻤﺮيء واﻟﻘﺮﺣﺔ‬
‫ وإﺻﺎﺑﺎت اﻟﻐﺸﺎء‬، (‫اﻟﻬﻀﻤﻴﺔ )اﻟﻤﻌﺪة واﻻﺛﻨﻲ ﻋﺸﺮ‬
‫ ﺗﻈﻬﺮ‬، ‫ ﻓﻲ ﺟﻤﻴﻊ ﻫﺬه اﻟﻈﺮوف‬.‫اﻟﻤﺨﺎﻃﻲ اﻟﻤﺮﺗﺒﻄﺔ ﺑﺎﻟﺘﻮﺗﺮ‬
‫ﺗﻘﺮﺣﺎت أو ﺗﻘﺮح اﻟﻐﺸﺎء اﻟﻤﺨﺎﻃﻲ ﻋﻨﺪﻣﺎ ﺗﻄﻐﻰ اﻟﺘﺄﺛﻴﺮات‬
Agents That Reduce Intragastric Acidity (‫ اﻟﺼﻔﺮاء‬، ‫ ﺑﻴﺒﺴﻴﻦ‬، ‫اﻟﻜﺎوﻳﺔ ﻟﻠﻌﻮاﻣﻞ اﻟﻌﺪواﻧﻴﺔ )ﺣﻤﺾ‬
‫ﻋﻠﻰ اﻟﻌﻮاﻣﻞ اﻟﺪﻓﺎﻋﻴﺔ ﻟﻠﻐﺸﺎء اﻟﻤﺨﺎﻃﻲ اﻟﻤﻌﺪي اﻟﻤﻌﻮي‬
1- ANTACIDS ‫ ﺗﺪﻓﻖ‬، ‫ اﻟﺒﺮوﺳﺘﺎﺟﻼﻧﺪﻳﻦ‬، ‫)إﻓﺮاز اﻟﻤﺨﺎط واﻟﺒﻴﻜﺮﺑﻮﻧﺎت‬
‫ وﻋﻤﻠﻴﺎت اﻻﺳﺘﻌﺎدة واﻟﺘﺠﺪﻳﺪ ﺑﻌﺪ اﻹﺻﺎﺑﺔ‬، ‫اﻟﺪم‬
.(‫اﻟﺨﻠﻮﻳﺔ‬

2-H2-RECEPTOR ANTAGONISTS
Four H2 antagonists are in clinical use:
Cimetidine , Ranitidine, Famotidine, and Nizatidine

The H2 antagonists exhibit competitive inhibition at the parietal cell


and suppress basal and meal-stimulated acid secretion in a linear, dose-
‫اﻟﻌﻮاﻣﻞ اﻟﺘﻲ ﺗﻘﻠﻞ ﻣﻦ ﺣﻤﻮﺿﺔ اﻟﻤﻌﺪة‬
dependent manner ‫ ﻣﻀﺎدات اﻟﺤﻤﻮﺿﺔ‬- 1

-H2 ‫ ﻣﺴﺘﻘﺒﻼت اﻟﺘﺤﻮﻻت‬-2


:‫ ﻗﻴﺪ اﻻﺳﺘﺨﺪام اﻟﺴﺮﻳﺮي‬H2 ‫أرﺑﻌﺔ ﻣﻀﺎدات‬
Clinical Uses ‫ ﻧﻴﺰاﺗﻴﺪﻳﻦ‬، ‫ ﻓﺎﻣﻮﺗﻴﺪﻳﻦ‬، ‫ راﻧﻴﺘﻴﺪﻳﻦ‬، ‫ﺳﻴﻤﻴﺘﻴﺪﻳﻦ‬

‫ﺗﻨﺎﻓﺴﻴﺎ ﻓﻲ اﻟﺨﻠﻴﺔ اﻟﺠﺪارﻳﺔ‬


ً ً
‫ﺗﺜﺒﻴﻄﺎ‬ H2 ‫ُﺗﻈﻬﺮ ﻣﻀﺎدات‬
A. Gastroesophageal Reflux Disease (Gerd) ‫وﺗﺜﺒﻂ إﻓﺮاز اﻟﺤﻤﺾ اﻟﻘﺎﻋﺪي واﻟﻤﺤﻔﺰ ﻟﻠﻮﺟﺒﺎت ﺑﻄﺮﻳﻘﺔ‬
‫ﺧﻄﻴﺔ ﺗﻌﺘﻤﺪ ﻋﻠﻰ اﻟﺠﺮﻋﺎت‬
B. Peptic Ulcer Disease
C. Nonulcer Dyspepsia ‫اﻻﺳﺘﺨﺪاﻣﺎت اﻟﺴﺮﻳﺮﻳﺔ‬
(‫ ﻣﺮض اﻟﺠﺰر اﻟﻤﻌﺪي اﻟﻤﺮﻳﺌﻲ )ﺟﻴﺮد‬.‫أ‬
D. Prevention Of Bleeding From Stress-Related Gastritis ‫ ﻣﺮض اﻟﻘﺮﺣﺔ اﻟﻬﻀﻤﻴﺔ‬.‫ب‬
‫ ﻋﺴﺮ اﻟﻬﻀﻢ اﻟﻼﻗﺮﺣﻲ‬.‫ج‬
‫ اﻟﻮﻗﺎﻳﺔ ﻣﻦ اﻟﻨﺰﻳﻒ اﻟﻨﺎﺗﺞ ﻋﻦ اﻟﺘﻬﺎب اﻟﻤﻌﺪة اﻟﻤﺮﺗﺒﻂ ﺑﺎﻟﺘﻮﺗﺮ‬.‫د‬

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PHARMACOLOGY Lec11---15 Dr.Labeeb
‫اﻵﺛﺎر اﻟﺴﻠﺒﻴﺔ‬
٪3 ‫ ﺗﺤﺪث اﻟﺘﺄﺛﻴﺮات اﻟﻀﺎﺋﺮة ﻓﻲ أﻗﻞ ﻣﻦ‬.‫ ﻋﻘﺎﻗﻴﺮ آﻣﻨﺔ ﻟﻠﻐﺎﻳﺔ‬H2 ‫ﻣﻀﺎدات‬
.‫ﻣﻦ اﻟﻤﺮﺿﻰ وﺗﺸﻤﻞ اﻹﺳﻬﺎل واﻟﺼﺪاع واﻟﺘﻌﺐ واﻷﻟﻢ اﻟﻌﻀﻠﻲ واﻹﻣﺴﺎك‬

Adverse Effects
H2 antagonists are extremely safe drugs. Adverse effects occur in fewer
than 3% of patients and include diarrhea, headache, fatigue, myalgias,
and constipation. ‫ وﻳﺜﺒﻂ اﺳﺘﻘﻼب‬، ‫ﻳﻤﻨﻊ اﻟﺴﻴﻤﻴﺘﻴﺪﻳﻦ ارﺗﺒﺎط ﺛﻨﺎﺋﻲ ﻫﻴﺪروﺗﺴﺘﻮﺳﺘﻴﺮون ﺑﻤﺴﺘﻘﺒﻼت اﻷﻧﺪروﺟﻴﻦ‬
‫ ﻋﻨﺪ اﺳﺘﺨﺪاﻣﻪ ﻋﻠﻰ اﻟﻤﺪى اﻟﻄﻮﻳﻞ أو‬.‫ وﻳﺰﻳﺪ ﻣﻦ ﻣﺴﺘﻮﻳﺎت اﻟﺒﺮوﻻﻛﺘﻴﻦ ﻓﻲ اﻟﺪم‬، ‫اﺳﺘﺮادﻳﻮل‬
.‫ ﻓﺈﻧﻪ ﻗﺪ ﻳﺴﺒﺐ اﻟﺘﺜﺪي أو اﻟﻀﻌﻒ اﻟﺠﻨﺴﻲ ﻟﺪى اﻟﺮﺟﺎل وﺳﻴﻼن اﻟﻠﺒﻦ ﻋﻨﺪ اﻟﻨﺴﺎء‬، ‫ﺑﺠﺮﻋﺎت ﻋﺎﻟﻴﺔ‬

Cimetidine inhibits binding of dihydrotestosterone to androgen


receptors, inhibits metabolism of estradiol, and increases serum
prolactin levels. When used long-term or in high doses, it may cause
gynecomastia or impotence in men and galactorrhea in women.

‫اﻟﺤﻤﻞ واﻟﺮﺿﺎﻋﺔ‬
.‫ﻻ ﻳﻨﺒﻐﻲ إﻋﻄﺎؤﻫﺎ ﻟﻠﺤﻮاﻣﻞ إﻻ ﻋﻨﺪ اﻟﻀﺮورة اﻟﻘﺼﻮى‬
PREGNANCY AND NURSING MOTHERS ‫ ﻓﻲ ﺣﻠﻴﺐ اﻟﺜﺪي وﺑﺎﻟﺘﺎﻟﻲ ﻗﺪ‬H2 ‫ﻳﺘﻢ إﻓﺮاز ﻣﻀﺎدات‬
ّ
.‫اﻟﺮﺿﻊ‬ ‫ﺗﺆﺛﺮ ﻋﻠﻰ‬

they should not be administered to pregnant women unless absolutely


necessary. The H2 antagonists are secreted into breast milk and may
therefore affect nursing infants.

Drug Interactions

Cimetidine interferes with several important hepatic cytochrome P450


drug metabolism pathways. Ranitidine binds 4-10 times less than
cimetidine to cytochrome P450. Negligible interaction occurs with
nizatidine and famotidine
‫ﺗﻔﺎﻋﻞ اﻷدوﻳﺔ‬
P450 ‫ﻳﺘﺪاﺧﻞ اﻟﺴﻴﻤﻴﺘﻴﺪﻳﻦ ﻣﻊ اﻟﻌﺪﻳﺪ ﻣﻦ ﻣﺴﺎرات اﻟﺘﻤﺜﻴﻞ اﻟﻐﺬاﺋﻲ ﻟﻌﻘﺎر اﻟﺴﻴﺘﻮﻛﺮوم‬
.P450 ‫ ﻣﺮات أﻗﻞ ﻣﻦ اﻟﺴﻴﻤﻴﺘﻴﺪﻳﻦ ﺑﺎﻟﺴﻴﺘﻮﻛﺮوم‬10-4 ‫ ﻳﺮﺗﺒﻂ راﻧﻴﺘﻴﺪﻳﻦ‬.‫اﻟﻜﺒﺪي‬
‫ﻳﺤﺪث ﺗﻔﺎﻋﻞ ﺿﺌﻴﻞ ﻣﻊ ﻧﻴﺰاﺗﻴﺪﻳﻦ وﻓﺎﻣﻮﺗﻴﺪﻳﻦ‬

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PHARMACOLOGY Lec11---15 Dr.Labeeb

3-PROTON PUMP INHIBITORS (PPI)

(PPI) ‫ﻣﺜﺒﻄﺎت ﻣﻀﺨﺔ اﻟﺒﺮوﺗﻮن‬-3


Five proton pump inhibitors are available for clinical use
‫ﺧﻤﺴﺔ ﻣﻦ ﻣﺜﺒﻄﺎت ﻣﻀﺨﺔ اﻟﺒﺮوﺗﻮن ﻣﺘﺎﺣﺔ ﻟﻼﺳﺘﺨﺪام اﻟﺴﺮﻳﺮي‬
Omeprazole ‫أوﻣﻴﺒﺮازول‬
‫ﻻﻧﺴﻮﺑﺮازول‬
Lansoprazole ‫راﺑﻴﺒﺮازول‬
‫ﺑﺎﻧﺘﻮﺑﺮازول‬
‫إﻳﺴﻮﻣﻴﺒﺮازول‬
Rabeprazole
‫ ﺗﺜﺒﻂ ﻣﺜﺒﻄﺎت ﻣﻀﺨﺔ اﻟﺒﺮوﺗﻮن ﻛﻼً ﻣﻦ اﻟﺼﻴﺎم‬، H2 ‫ﻋﻠﻰ ﻋﻜﺲ ﻣﻀﺎدات‬
Pantoprazole .‫واﻹﻓﺮاز اﻟﺬي ﻳﺤﻔﺰه اﻟﻄﻌﺎم ﻷﻧﻬﺎ ﺗﻤﻨﻊ اﻟﻤﺴﺎر اﻟﻤﺸﺘﺮك اﻟﻨﻬﺎﺋﻲ ﻹﻓﺮاز اﻟﺤﻤﺾ‬

Esomeprazole

In contrast to H2 antagonists, proton pump inhibitors inhibit


both fasting and meal-stimulated secretion because they block
the final common pathway of acid secretion
‫اﻻﺳﺘﺨﺪاﻣﺎت اﻟﺴﺮﻳﺮﻳﺔ‬
(‫ﻣﺮض اﻟﺠﺰر اﻟﻤﻌﺪي اﻟﻤﺮﻳﺌﻲ )ﺟﻴﺮد‬.‫أ‬
‫ ﻣﺮض اﻟﻘﺮﺣﺔ اﻟﻬﻀﻤﻴﺔ‬-‫ب‬
Clinical Uses ‫ اﻟﻘﺮﺣﺔ اﻟﻤﺼﺎﺣﺒﺔ‬-‫ ﻣﻀﺎدات اﻻﻟﺘﻬﺎب ﻏﻴﺮ اﻟﺴﺘﻴﺮوﺋﻴﺪﻳﺔ‬-‫ج‬
.‫ ﻋﺴﺮ اﻟﻬﻀﻢ اﻟﻼﻗﺮﺣﻲ‬-‫د‬
A. Gastroesophageal Reflux Disease (Gerd)
B. Peptic Ulcer Disease
C. NSAID- Associated Ulcers
D. Nonulcer Dyspepsia.

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PHARMACOLOGY Lec11---15 Dr.Labeeb

‫ﻋﻮاﻣﻞ ﺣﻤﺎﻳﺔ اﻷﻏﺸﻴﺔ اﻟﻤﺨﺎﻃﻴﺔ‬


‫ﺳﻮﻛﺮاﻟﻔﺎت‬
MUCOSAL PROTECTIVE AGENTS
.‫ﻧﻈﺎﺋﺮ اﻟﺒﺮوﺳﺘﺎﺟﻼﻧﺪﻳﻦ‬
Sucralfate ‫ﻳﺤﺘﻮي اﻟﻤﻴﺰوﺑﺮوﺳﺘﻮل ﻋﻠﻰ ﺧﺼﺎﺋﺺ ﻣﺜﺒﻄﺔ ﻟﻸﺣﻤﺎض وﺧﺼﺎﺋﺺ‬
.‫واﻗﻴﺔ ﻣﻦ اﻟﻐﺸﺎء اﻟﻤﺨﺎﻃﻲ‬

‫ﻣﺮﻛﺒﺎت اﻟﺒﺰﻣﻮت اﻟﻐﺮوﻳﺔ‬

Prostaglandin Analogs
Misoprostol has both Acid Inhibitory And Mucosal Protective
Properties..

Colloidal Bismuth Compounds

Antispasmodics (Anticholinergics)

Agents are promoted as providing relief of abdominal pain or


discomfort through antispasmodic actions.
These agents work primarily through anticholinergic activities.
Commonly used medications in this class include hyoscyamine.
These drugs inhibit muscarinic cholinergic receptors in the enteric
plexus and on smooth muscle.
At low doses, they have minimal autonomic effects.
However, at higher doses they exhibit significant additional
anticholinergic effects, including dry mouth, visual disturbances,
urinary retention, and constipation. (‫ﻣﻀﺎدات اﻟﺘﺸﻨﺞ )ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ‬

‫ﻳﺘﻢ اﻟﺘﺮوﻳﺞ ﻟﻬﺎ ﻋﻠﻰ أﻧﻬﺎ ﺗﺨﻔﻒ ﻣﻦ آﻻم اﻟﺒﻄﻦ أو‬


.‫ﻋﺪم اﻟﺮاﺣﺔ ﻣﻦ ﺧﻼل اﻹﺟﺮاءات اﻟﻤﻀﺎدة ﻟﻠﺘﺸﻨﺞ‬
.‫ﺗﻌﻤﻞ ﻫﺬه اﻟﻌﻮاﻣﻞ ﺑﺸﻜﻞ أﺳﺎﺳﻲ ﻣﻦ ﺧﻼل أﻧﺸﻄﺔ ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ‬
.‫ﺗﺸﻤﻞ اﻷدوﻳﺔ اﻟﻤﺴﺘﺨﺪﻣﺔ ﺑﺸﻜﻞ ﺷﺎﺋﻊ ﻓﻲ ﻫﺬه اﻟﻔﺌﺔ ﻫﻴﻮﺳﻴﺎﻣﻴﻦ‬
‫ﺗﺜﺒﻂ ﻫﺬه اﻷدوﻳﺔ اﻟﻤﺴﺘﻘﺒﻼت اﻟﻜﻮﻟﻴﻨﻴﺔ اﻟﻤﺴﻜﺎرﻳﻨﻴﺔ ﻓﻲ اﻷﻣﻌﺎء‬
.‫اﻟﻀﻔﻴﺮة واﻟﻌﻀﻼت اﻟﻤﻠﺴﺎء‬
.‫ ﻳﻜﻮن ﻟﻬﺎ ﺗﺄﺛﻴﺮات ذاﺗﻴﺔ ﻗﻠﻴﻠﺔ‬، ‫ﻋﻨﺪ اﻟﺠﺮﻋﺎت اﻟﻤﻨﺨﻔﻀﺔ‬
‫ ﺑﻤﺎ ﻓﻲ‬، ‫ ﻓﺈﻧﻬﺎ ﺗﻈﻬﺮ ﻋﻨﺪ اﻟﺠﺮﻋﺎت اﻟﻌﺎﻟﻴﺔ ﺗﺄﺛﻴﺮات إﺿﺎﻓﻴﺔ ﻛﺒﻴﺮة ﻟﻤﻀﺎدات اﻟﻜﻮﻟﻴﻦ‬، ‫وﻣﻊ ذﻟﻚ‬
.‫ واﻹﻣﺴﺎك‬، ‫ واﺣﺘﺒﺎس اﻟﺒﻮل‬، ‫ واﻻﺿﻄﺮاﺑﺎت اﻟﺒﺼﺮﻳﺔ‬، ‫ذﻟﻚ ﺟﻔﺎف اﻟﻔﻢ‬
XIII
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ﻗﺪ ﻳﻜﻮن اﻟﻐﺜﻴﺎن واﻟﻘﻲء ﻣﻦ ﻣﻈﺎﻫﺮ ﻣﺠﻤﻮﻋﺔ ﻣﺘﻨﻮﻋﺔ ﻣﻦ اﻟﺤﺎﻻت )اﻵﺛﺎر اﻟﺴﻠﺒﻴﺔ ﻣﻦ‬
‫ﻣﻀﺎد اﻟﻘﻲء‬ ‫ ﻋﺪوى اﻟﺠﻬﺎز‬، ‫ ﺿﻌﻒ اﻟﺠﻬﺎز اﻟﺪﻫﻠﻴﺰي‬، ‫ اﻟﺤﻤﻞ‬، ‫ اﻻﺿﻄﺮاﺑﺎت اﻟﺠﻬﺎزﻳﺔ أو اﻟﻌﺪوى‬، ‫اﻷدوﻳﺔ‬
‫ اﻟﻌﻼج‬، ‫ اﺿﻄﺮاﺑﺎت اﻟﻜﺒﺪ اﻟﺼﻔﺮاوي‬، ‫ اﻟﺘﻬﺎب اﻟﺼﻔﺎق‬، ‫اﻟﻌﺼﺒﻲ اﻟﻤﺮﻛﺰي أو زﻳﺎدة اﻟﻀﻐﻂ‬
ANTI EMETIC ‫ أو اﻻﻟﺘﻬﺎﺑﺎت‬، ‫ ﺧﻠﻞ اﻟﺤﺮﻛﺔ‬، ‫ اﻧﺴﺪاد اﻟﺠﻬﺎز اﻟﻬﻀﻤﻲ‬، ‫اﻹﺷﻌﺎﻋﻲ أو اﻟﻜﻴﻤﻴﺎﺋﻲ‬

Nausea and vomiting may be manifestations of a wide variety of


conditions( adverse effects from medications; systemic disorders or
infections; pregnancy; vestibular dysfunction; CNS infection or
increased pressure; peritonitis; hepatobiliary disorders; radiation or
chemotherapy; and gastrointestinal obstruction, dysmotility, or
‫ ﻫﺬه اﻟﻌﻮاﻣﻞ ﺗﺰﻳﺪ ﻣﻦ ﺳﻌﺔ اﻟﻤﺮيء‬.. D2 ‫ﻣﻴﺘﻮﻛﻠﻮﺑﺮاﻣﻴﺪ ودوﻣﺒﻴﺮﻳﺪون ﻫﻤﺎ ﻣﻦ ﻣﻀﺎدات ﻣﺴﺘﻘﺒﻼت اﻟﺪوﺑﺎﻣﻴﻦ‬
infections ‫ ﻳﺤﺠﺐ ﻣﻴﺘﻮﻛﻠﻮﺑﺮاﻣﻴﺪ ودوﻣﺒﻴﺮﻳﺪون‬.‫ وﺗﻌﺰز إﻓﺮاغ اﻟﻤﻌﺪة‬، ‫ وﺗﺰﻳﺪ ﻣﻦ ﺿﻐﻂ اﻟﻌﻀﻠﺔ اﻟﻌﺎﺻﺮة ﻟﻠﻤﺮيء‬، ‫اﻟﺘﻤﻌﺠﻴﺔ‬
ً
‫ ﻣﻤﺎ ﻳﺆدي إﻟﻰ ﺗﺄﺛﻴﺮ ﻣﻀﺎد‬، ‫ ﻓﻲ ﻣﻨﻄﻘﺔ ﺗﺤﻔﻴﺰ اﻟﻤﺴﺘﻘﺒﻼت اﻟﻜﻴﻤﻴﺎﺋﻴﺔ ﻓﻲ اﻟﻨﺨﺎع‬D2 ‫أﻳﻀﺎ ﻣﺴﺘﻘﺒﻼت اﻟﺪوﺑﺎﻣﻴﻦ‬
.‫ﻟﻠﻐﺜﻴﺎن وﻣﻀﺎد ﻟﻠﻘﻰء‬
Metoclopramide and domperidone are dopamine D2 receptor
antagonists.. These agents increase esophageal peristaltic amplitude,
increase lower esophageal sphincter pressure, and enhance gastric
emptying. Metoclopramide and domperidone also block dopamine D2
receptors in the chemoreceptor trigger zone of the medulla, resulting in
potent antinausea and antiemetic action.
Clinical Uses
‫اﻻﺳﺘﺨﺪاﻣﺎت اﻟﺴﺮﻳﺮﻳﺔ‬
A. Gastroesophageal Reflux Disease (Gerd) (‫ ﻣﺮض اﻟﺠﺰر اﻟﻤﻌﺪي اﻟﻤﺮﻳﺌﻲ )ﺟﻴﺮد‬.‫أ‬
‫ اﺧﺘﻼل إﻓﺮاغ اﻟﻤﻌﺪة‬.‫ب‬
.‫ ﻋﺴﺮ اﻟﻬﻀﻢ ﻏﻴﺮ اﻟﺘﻘﺮﺣﻲ‬.‫ج‬
B. Impaired Gastric Emptying .‫ اﻟﻮﻗﺎﻳﺔ ﻣﻦ اﻟﻘﻲء‬-‫د‬
‫ ﺗﺤﻔﻴﺰ اﻟﺮﺿﺎﻋﺔ ﺑﻌﺪ اﻟﻮﻻدة‬.‫ه‬
C. Nonulcer Dyspepsia.
D. Prevention Of Vomiting
E. Postpartum Lactation Stimulation
Adverse Effects
The most common adverse effects of metoclopramide involve the
Restlessness, drowsiness, insomnia, anxiety, and agitation occur
especially the elderly Elevated prolactin levels can cause
galactorrhea,gynecomastia, impotence, and menstrual disorders.
‫اﻵﺛﺎر اﻟﺴﻠﺒﻴﺔ‬
‫ﺗﺸﻤﻞ اﻵﺛﺎر اﻟﺠﺎﻧﺒﻴﺔ اﻷﻛﺜﺮ ﺷﻴﻮﻋً ﺎ ﻟﻠﻤﻴﺘﻮﻛﻠﻮﺑﺮاﻣﻴﺪ اﻟﺘﻤﻠﻤﻞ واﻟﻨﻌﺎس واﻷرق‬
‫ﺧﺎﺻﺔ ﻋﻨﺪ ﻛﺒﺎر اﻟﺴﻦ ﻳﻤﻜﻦ أن ﺗﺴﺒﺐ ﻣﺴﺘﻮﻳﺎت اﻟﺒﺮوﻻﻛﺘﻴﻦ‬ ً ‫واﻟﻘﻠﻖ واﻹﺛﺎرة‬
.‫اﻟﻤﺮﺗﻔﻌﺔ ﺛﺮ اﻟﻠﺒﻦ واﻟﺘﺜﺪي واﻟﻌﺠﺰ اﻟﺠﻨﺴﻲ واﺿﻄﺮاﺑﺎت اﻟﺪورة اﻟﺸﻬﺮﻳﺔ‬
XIV
‫اﻟﻤﻠﻴﻨﺎت اﻟﺘﻲ ﺗﺘﺸﻜﻞ ﺑﻜﻤﻴﺎت ﻛﺒﻴﺮة ﻣﻦ اﻟﻐﺮوﻳﺎت ﻏﻴﺮ اﻟﻘﺎﺑﻠﺔ ﻟﻠﻬﻀﻢ واﻟﺘﻲ ﺗﻤﺘﺺ اﻟﻤﺎء‬
ً ‫وﺗﺸﻜﻞ‬
‫ ﺗﺸﻤﻞ اﻟﻤﺴﺘﺤﻀﺮات‬.‫ﺟﻼ ﻣﺮﻃ ًﺒﺎ ﺿﺨﻤً ﺎ ﻳﻌﻤﻞ ﻋﻠﻰ ﺗﻤﺪد اﻟﻘﻮﻟﻮن وﻳﻌﺰز اﻟﺘﻤﻌﺞ‬
‫ ﻣﻴﺜﻴﻞ ﺳﻠﻮﻟﻮز( واﻷﻟﻴﺎف اﻻﺻﻄﻨﺎﻋﻴﺔ‬،) ‫اﻟﺸﺎﺋﻌﺔ اﻟﻤﻨﺘﺠﺎت اﻟﻨﺒﺎﺗﻴﺔ اﻟﻄﺒﻴﻌﻴﺔ‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫اﻟﻤﻠﻴﻨﺎت‬ LAXATIVES
Bulk-Forming Laxatives indigestible, hydrophilic colloids that
absorb water, forming a bulky, emollient gel that distends the colon and
promotes peristalsis. Common preparations include natural plant
products (, methylcellulose) and synthetic fibers
‫ ﻣﻤﺎ‬، ‫ﻋﻮاﻣﻞ اﻟﻔﺎﻋﻞ ﺑﺎﻟﺴﻄﺢ ﻓﻲ اﻟﺒﺮاز )اﻟﻤﻠﻴﻨﺎت( ﺗﻌﻤﻞ ﻫﺬه اﻟﻌﻮاﻣﻞ ﻋﻠﻰ ﺗﻠﻴﻴﻦ ﻣﺎدة اﻟﺒﺮاز‬
.. ‫ وﺗﺸﻤﻞ اﻟﻌﻮاﻣﻞ اﻟﺸﺎﺋﻌﺔ ﺗﺤﺎﻣﻴﻞ اﻟﺠﻠﺴﺮﻳﻦ‬.. ‫ﻳﺴﻤﺢ ﻟﻠﻤﺎء واﻟﺪﻫﻮن ﺑﺎﻟﺘﻐﻠﻐﻞ‬

Stool Surfactant Agents (Softeners) These agents soften stool


material, permitting water and lipids to penetrate.. Common agents
include glycerin suppository.. ‫ اﻟﺴﻜﺮﻳﺎت أو اﻷﻣﻼح ﻏﻴﺮ اﻟﻘﺎﺑﻠﺔ ﻟﻼﻣﺘﺼﺎص‬:‫اﻟﻤﻠﻴﻨﺎت اﻷﺳﻤﻮزﻳﺔ‬
‫ﻳﻤﻜﻦ اﺳﺘﺨﺪام ﻫﺬه اﻟﻌﻮاﻣﻞ ﻓﻲ ﻋﻼج اﻹﻣﺴﺎك اﻟﺤﺎد أو ﻋﻼج اﻹﻣﺴﺎك‬
.‫ اﻟﻤﺴﻬﻼت اﻟﺸﺎﺋﻌﺔ ﻫﻲ ﺳﺘﺮات اﻟﻤﻐﻨﻴﺴﻴﻮم وﻓﻮﺳﻔﺎت اﻟﺼﻮدﻳﻮم‬.‫ﻣﻨﻊ اﻹﻣﺴﺎك اﻟﻤﺰﻣﻦ‬

Osmotic Laxatives :Non absorbable Sugars or Salts


These agents may be used for the treatment of acute constipation or the
prevention of chronic constipation. The commonly purgatives are
magnesium citrate and sodium phosphate.

.(‫اﻟﻤﻠﻴﻨﺎت اﻟﻤﻨﺒﻬﺔ )اﻟﻤﺴﻬﻼت‬


Stimulant Laxatives(Cathartic). ‫اﻟﻤﻠﻴﻨﺎت اﻟﻤﻨﺒﻬﺔ )اﻟﻤﺴﻬﻼت( ﺗﺤﻔﺰ ﺣﺮﻛﺔ اﻷﻣﻌﺎء ﻣﻦ ﺧﻼل‬
.‫ﻋﺪد ﻣﻦ اﻵﻟﻴﺎت ﻏﻴﺮ اﻟﻤﻔﻬﻮﻣﺔ ﺟﻴﺪً ا‬

Stimulant laxatives (cathartics) induce bowel movements through a


number of poorly understood mechanisms.
‫ ﻳﺘﻢ‬.‫ﻣﺸﺘﻘﺎت اﻷﻧﺜﺮاﻛﻴﻨﻮن اﻟﺼﺒﺎر واﻟﺴﻨﺎ واﻟﻜﺴﻜﺎرا ﺗﺤﺪث ﺑﺸﻜﻞ ﻃﺒﻴﻌﻲ ﻓﻲ اﻟﻨﺒﺎﺗﺎت‬
‫ ﺗﻨﺘﺞ ﺣﺮﻛﺔ اﻷﻣﻌﺎء‬، ‫اﻣﺘﺼﺎص ﻫﺬه اﻟﻤﻠﻴﻨﺎت ﺑﺸﻜﻞ ﺳﻴﺊ وﺑﻌﺪ اﻟﺘﺤﻠﻞ اﻟﻤﺎﺋﻲ ﻓﻲ اﻟﻘﻮﻟﻮن‬
Anthraquinone Derivatives Aloe, senna, and cascara occur naturally
in plants. These laxatives are poorly absorbed and after hydrolysis in
the colon, produce a bowel movement

Castor Oil Formerly used as a purgative to clean the colon before


procedures, it is now seldom used.
ً
، ‫ﺳﺎﺑﻘﺎ ﻛﻤﺴﻬﻞ ﻟﺘﻨﻈﻴﻒ اﻟﻘﻮﻟﻮن ﻗﺒﻞ اﻹﺟﺮاءات‬ ‫زﻳﺖ اﻟﺨﺮوع ﻛﺎن ﻳُ ﺴﺘﺨﺪم‬
Biscodel stimulated bowel .‫وﻧﺎدرً ا ﻣﺎ ﻳﺴﺘﺨﺪم اﻵن‬

‫ﺑﻴﺴﻜﻮدل ﺗﺤﻔﻴﺰ اﻷﻣﻌﺎء‬

XV
‫ﻳﻤﻜﻦ اﺳﺘﺨﺪام اﻟﻌﻮاﻣﻞ اﻟﻤﻀﺎدة ﻟﻺﺳﻬﺎل ﺑﺄﻣﺎن ﻓﻲ اﻟﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﻌﺎﻧﻮن ﻣﻦ اﻹﺳﻬﺎل‬
‫ ﻻ ﻳﻨﺒﻐﻲ أن ﺗﺴﺘﺨﺪم ﻓﻲ‬، ‫ وﻣﻊ ذﻟﻚ‬.‫اﻟﺨﻔﻴﻒ إﻟﻰ اﻟﻤﺘﻮﺳﻂ اﻟﺤﺎد‬
PHARMACOLOGY Lec11---15 Dr.Labeeb
‫ﻋﻮاﻣﻞ ﻣﻀﺎد ﻟﻺﺳﻬﺎل‬ ‫ أو اﻟﺴﻤﻴﺔ اﻟﺠﻬﺎزﻳﺔ‬، ‫ وارﺗﻔﺎع ﻓﻲ درﺟﺔ اﻟﺤﺮارة‬، ‫اﻟﻤﺮﺿﻰ اﻟﺬﻳﻦ ﻳﻌﺎﻧﻮن ﻣﻦ اﻹﺳﻬﺎل اﻟﺪﻣﻮي‬
‫ ﻛﻤﺎ ﺗﺴﺘﺨﺪم ﻣﻀﺎدات اﻹﺳﻬﺎل ﻟﻠﺴﻴﻄﺮة ﻋﻠﻰ اﻹﺳﻬﺎل‬.‫ﺑﺴﺒﺐ ﺧﻄﺮ ﺗﻔﺎﻗﻢ اﻟﺤﺎﻟﺔ اﻷﺳﺎﺳﻴﺔ‬
Antidiarrheal Agents .(IBD) ‫( أو ﻣﺮض اﻟﺘﻬﺎب اﻷﻣﻌﺎء‬IBS) ‫اﻟﻤﺰﻣﻦ اﻟﻨﺎﺟﻢ ﻋﻦ ﺣﺎﻻت ﻣﺜﻞ ﻣﺘﻼزﻣﺔ اﻟﻘﻮﻟﻮن اﻟﻌﺼﺒﻲ‬

Antidiarrheal agents may be used safely in patients with mild to


moderate acute diarrhea. However, they should not be used in patients
with bloody diarrhea, high fever, or systemic toxicity because of the
risk of worsening the underlying condition.. Antidiarrheals are also
used to control chronic diarrhea caused by such conditions as irritable
bowel syndrome (IBS) or inflammatory bowel disease (IBD).
‫أﻓﻴﻮﻧﻴﺎت اﻟﻤﻔﻌﻮل‬
‫ﻟﻬﺎ ﺗﺄﺛﻴﺮات إﻣﺴﺎك ﻛﺒﻴﺮة )زﻳﺎدة وﻗﺖ ﻋﺒﻮر اﻟﻘﻮﻟﻮن واﻣﺘﺼﺎص اﻟﻤﺎء ﻓﻲ‬
.‫ ﻛﻤﺎ أﻧﻬﺎ ﺗﻘﻠﻞ ﻣﻦ ﺣﺮﻛﺎت اﻟﻘﻮﻟﻮن اﻟﺠﻤﺎﻋﻴﺔ وردود اﻟﻤﻌﺪة اﻟﻤﻌﻮﻳﺔ‬، ‫اﻟﺒﺮاز‬
Opioids ‫ﻟﻮﺑﻴﺮاﻣﻴﺪ ﻫﻮ ﻧﺎﻫﺾ أﻓﻴﻮﻧﻲ ﺑﺪون وﺻﻔﺔ ﻃﺒﻴﺔ ﻻ ﻳﻌﺒﺮ اﻟﺤﺎﺟﺰ اﻟﺪﻣﻮي‬
.‫اﻟﺪﻣﺎﻏﻲ وﻟﻴﺲ ﻟﻪ ﺧﺼﺎﺋﺺ ﻣﺴﻜﻨﺔ أو اﺣﺘﻤﺎﻟﻴﺔ ﻟﻺدﻣﺎن‬

have significant constipating effects (increased colonic transit time and


fecal water absorption. They also decrease mass colonic movements
and the gastrocolic reflex.Loperamide is a nonprescription opioid
agonist that does not cross the blood-brain barrier and has no analgesic
properties or potential for addiction.
. Commercial preparations commonly contain small amounts of
atropine to discourage overdosage (2.5 mg diphenoxylate with 0.025
mg atropine). The anticholinergic properties of atropine may contribute
‫ﺗﺤﺘﻮي اﻟﻤﺴﺘﺤﻀﺮات اﻟﺘﺠﺎرﻳﺔ ﻋﺎدة ﻋﻠﻰ ﻛﻤﻴﺎت ﺻﻐﻴﺮة ﻣﻦ اﻷﺗﺮوﺑﻴﻦ ﻟﺘﺜﺒﻴﻂ‬
to the antidiarrheal action. ‫ ﻗﺪ‬.(‫ ﻣﺠﻢ أﺗﺮوﺑﻴﻦ‬0.025 ‫ ﻣﺠﻢ دﻳﻔﻴﻨﻮﻛﺴﻴﻼت ﻣﻊ‬2.5) ‫اﻟﺠﺮﻋﺔ اﻟﺰاﺋﺪة‬
.‫ﺗﺴﺎﻫﻢ ﺧﺼﺎﺋﺺ اﻷﺗﺮوﺑﻴﻦ اﻟﻤﻀﺎدة ﻟﻠﻜﻮﻟﻴﻦ ﻓﻲ اﻟﺘﺄﺛﻴﺮ اﻟﻤﻀﺎد ﻟﻺﺳﻬﺎل‬

Colloidal Bismuth Compounds


Kaolin is a naturally occurring hydrated magnesium aluminum silicate,
and pectin is an indigestible carbohydrate derived from apples. Both
appear to act as absorbents of bacteria, toxins, and fluid, thereby
decreasing stool liquidity and number. ‫ﻣﺮﻛﺒﺎت اﻟﺒﺰﻣﻮت اﻟﻐﺮوﻳﺔ‬
، ‫ﻃﺒﻴﻌﻴﺎ‬
ً ‫اﻟﻜﺎوﻟﻴﻦ ﻋﺒﺎرة ﻋﻦ ﺳﻴﻠﻴﻜﺎت أﻟﻮﻣﻨﻴﻮم ﻣﻐﻨﻴﺴﻴﻮم رﻃﺐ‬
.‫واﻟﺒﻜﺘﻴﻦ ﻫﻮ ﻛﺮﺑﻮﻫﻴﺪرات ﻏﻴﺮ ﻗﺎﺑﻠﺔ ﻟﻠﻬﻀﻢ ﻣﺸﺘﻘﺔ ﻣﻦ اﻟﺘﻔﺎح‬
، ‫ﻳﺒﺪو أن ﻛﻼﻫﻤﺎ ﻳﻌﻤﻞ ﻛﻤﻤﺘﺺ ﻟﻠﺒﻜﺘﻴﺮﻳﺎ واﻟﺴﻤﻮم واﻟﺴﻮاﺋﻞ‬
.‫وﺑﺎﻟﺘﺎﻟﻲ ﻳﻘﻠﻞ ﻣﻦ ﺳﻴﻮﻟﺔ اﻟﺒﺮاز وﻋﺪده‬
XVI
*bloating,
‫ﺣﺎﻟﺔ ﻣﻨﺘﻔﺨﺔ ﻧﺎﺗﺠﺔ ﻋﻦ‬
‫اﺣﺘﺒﺎس اﻟﺴﻮاﺋﻞ أو‬
.‫اﻟﻐﺎزات‬

PHARMACOLOGY Lec11---15 Dr.Labeeb


‫( ﻫﻲ اﺿﻄﺮاب ﻣﺰﻣﻦ ﻣﺠﻬﻮل اﻟﺴﺒﺐ ﻳﺘﺴﻢ ﺑﺎﻧﺰﻋﺎج‬IBS) ‫ﻣﺘﻼزﻣﺔ اﻟﻘﻮﻟﻮن اﻟﻌﺼﺒﻲ‬
.‫ﻋﻼج اﻟﻘﻮﻟﻮن اﻟﻌﺼﺒﻲ‬ ‫ أو ﺗﻘﻠﺼﺎت( ﻣﻘﺘﺮﻧﺔ ﺑﺎﻟﺘﻐﻴﺮات ﻓﻲ ﻋﺎدات‬، ‫ أو اﻧﺘﻔﺎخ‬، ‫ أو اﻧﺘﻔﺎخ‬، ‫ﻓﻲ اﻟﺒﻄﻦ )أﻟﻢ‬
The Treatment Of Irritable Bowel Syndrome. (‫ أو ﻛﻠﻴﻬﻤﺎ‬، ‫ أو اﻹﻣﺴﺎك‬، ‫اﻷﻣﻌﺎء )اﻹﺳﻬﺎل‬

Irritable bowel syndrome (IBS) is an idiopathic chronic, relapsing


disorder characterized by abdominal discomfort (pain, bloating,
distention, or cramps) in association with alterations in bowel habits
‫اﻟﻌﻼﺟﺎت اﻟﺪواﺋﻴﺔ اﻟﻤﻮﺟﻬﺔ ﻟﺘﺨﻔﻴﻒ آﻻم اﻟﺒﻄﻦ وﻋﺪم اﻟﺮاﺣﺔ وﺗﺤﺴﻴﻦ وﻇﻴﻔﺔ‬
(diarrhea, constipation, or both) ‫ ﻳﺒﺪو أن اﻟﺠﺮﻋﺎت اﻟﻤﻨﺨﻔﻀﺔ ﻣﻦ ﻣﻀﺎدات‬، ‫ ﻟﻌﻼج آﻻم اﻟﺒﻄﻦ اﻟﻤﺰﻣﻨﺔ‬.‫اﻷﻣﻌﺎء‬
‫اﻻﻛﺘﺌﺎب ﺛﻼﺛﻴﺔ اﻟﺤﻠﻘﺎت )ﻣﺜﻞ أﻣﻴﺘﺮﻳﺒﺘﻴﻠﻴﻦ أو دﻳﺴﻴﺒﺮاﻣﻴﻦ( ﻣﻔﻴﺪة‬
.
Pharmacologic therapies directed at relieving abdominal pain and
discomfort and improving bowel function.For the treatment of chronic
abdominal pain, low doses of tricyclic antidepressants (eg,
amitriptyline or desipramine, appear to be helpful . The anticholinergic
properties of these agents also may have effects on gastrointestinal
motility and secretion, reducing stool frequency and liquidity of stools
ً
‫أﻳﻀﺎ ﺗﺄﺛﻴﺮات ﻋﻠﻰ ﺣﺮﻛﻴﺔ‬ ‫ﻣﻀﺎدات اﻟﻜﻮﻟﻴﻦ ﻗﺪ ﻳﻜﻮن ﻟﺨﺼﺎﺋﺺ ﻫﺬه اﻟﻌﻮاﻣﻞ‬
‫ ﻣﻤﺎ ﻳﻘﻠﻞ ﻣﻦ ﺗﻮاﺗﺮ اﻟﺒﺮاز وﺳﻴﻮﻟﺔ اﻟﺒﺮاز‬، ‫اﻟﺠﻬﺎز اﻟﻬﻀﻤﻲ وإﻓﺮازه‬

Drugs Treat Inflammatorybowel Disease


Inflammatory bowel disease (IBD) comprises two distinct disorders:
ulcerative colitis and Crohn's disease.
1- Aminosalicylates
Drugs that contain 5-aminosalicylic acid (5-ASA) have been used
successfully for decades in the treatment of inflammatory bowel
diseases.
A. Azo Compounds Sulfasalazine, balsalazide, and olsalazine
B. Mesalamine Compounds
2- Purine Analogs: Azathioprine & 6-Mercaptopurine
‫اﻷدوﻳﺔ ﺗﻌﺎﻟﺞ ﻣﺮض اﻟﺘﻬﺎب اﻷﻣﻌﺎء‬
3- Methotrexate :‫( ﻋﻠﻰ ﻧﻮﻋﻴﻦ ﻣﺨﺘﻠﻔﻴﻦ ﻣﻦ اﻻﺿﻄﺮاﺑﺎت‬IBD) ‫ﻳﺸﺘﻤﻞ ﻣﺮض اﻟﺘﻬﺎب اﻷﻣﻌﺎء‬
.‫اﻟﺘﻬﺎب اﻟﻘﻮﻟﻮن اﻟﺘﻘﺮﺣﻲ وﻣﺮض ﻛﺮون‬

‫ أﻣﻴﻨﻮﺳﺎﻟﻴﺴﻴﻼت‬-1
(ASA-5) ‫أﻣﻴﻨﻮﺳﺎﻟﻴﺴﻴﻠﻴﻚ‬-5 ‫ﺗﻢ اﺳﺘﺨﺪام اﻷدوﻳﺔ اﻟﺘﻲ ﺗﺤﺘﻮي ﻋﻠﻰ ﺣﻤﺾ‬
.‫ﺑﻨﺠﺎح ﻟﻌﻘﻮد ﻣﻦ اﻟﺰﻣﻦ ﻓﻲ ﻋﻼج أﻣﺮاض اﻷﻣﻌﺎء اﻻﻟﺘﻬﺎﺑﻴﺔ‬
‫ ﺑﻠﺴﺎﻻزﻳﺪ وأوﻟﺴﺎﻻزﻳﻦ‬، ‫ ﺳﻠﻔﺎﺳﺎﻻزﻳﻦ‬:‫ﻣﺮﻛﺒﺎت آزو‬.‫أ‬
XVII ‫ﻣﺮﻛﺒﺎت ﻣﻴﺴﺎﻻﻣﻴﻦ‬.‫ب‬

‫ﻣﻴﺮﻛﺎﺑﺘﻮﺑﻮرﻳﻦ‬-6 ‫ أزاﺛﻴﻮﺑﺮﻳﻦ و‬:‫ ﻧﻈﺎﺋﺮ اﻟﺒﻴﻮرﻳﻦ‬-2

‫ ﻣﻴﺜﻮﺗﺮﻳﻜﺴﺎت‬-3

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