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رسالة المركز

العدد التاسع

في هذا العدد


CESSATION OF SMOKING BY USING ZYBAN ORALLY

 

الإقلاع عن التدخين باستخدام عقار زيبان

 

DOXOFYLLINE: A NEW GENERATION XANTHINE BRONCHODILATOR

 

دوكسيفيللين عقار جديد موسع للشعب الهوائية

 

KOLA NUT IS LIFE

 

جوزة الكولا (القورو) هي الحياة

 

VENOM FROM MARINE SNAILS FIGHTS AGAINST CANCER PAIN

 

سم القواقع البحرية يقضي على آلام السرطان

 

CESSATION OF SMOKING BY USING ZYBAN ORALLY

    

     Bupropion hydrochloride (zyban )is an antidepressant phenyl–butamine of aminoketone class chemically unrelated to tricyclic, tetracyclic or other currently available antidepressants (e.g. selective serotonin-reuptake inhibitors).

Mechanism of action:

     Bupropion is not a monoamine oxidase inhibitor, exerts effect on 5-hydroxytryptamine uptake, and minimally alters the reuptake of norepinephrine at presynaptic sites. It is a weak inhibitor of dopamine reuptake,but its mechanism of action has not been clarified.
The precise mechanism of action responsible for the efficacy of Bupropion as an adjunct in the cessation of smoking is unclear although reuptake inhibition of noradrenaline and dopamine is involved, it has been suggested that central nervous system (CNS) effects of dopamine might be involved in the reinforcement properties of addictive drugs and that nicotine withdrawal manifestations involve the absence of CNS effects of norepinefrine that is mediated by nicotine.
Efficacy of bupropion in smoking cessation does not appear to depend on the presence of underlying depression.

Therapeutic doses:

1-for major depression:

     The initial dosage ranges up to 200mg/d in divided amount. After a three days of treatment, the dosage of bupropion in adults may be increased to 100mg three times daily. After several weeks of treatment, in patients in whom no clinical improvement is seen, the dosage may be increased gradually to 450mg/d given in divided doses of more than 150mgeach, provided that there is clinical improvement at this level. If not, bupropion is then discontinued.

2-For smoking cessation:

     For use in adults as an adjunct in smoking  cessation,  the initial dosage of bupropion hydrochloride is 150mg daily for the first 3 days of therapy. The dosage is subsequently increased in most patients to the usual recommended dosage of 150mg twice daily, which is also the maximum recommended dosage. Dosages exceeding 300 mg daily should not be used for smoking cessation because of the risk of seizures. Patients should continue to receive bupropion hydrochloride for 7-12 weeks. Discontinuation of therapy does not require tapering of the dosage.
     Authors have reported that about 30.3% of smokers treated with zyban stopped smoking within a year, and that zyban has been twice more effective than nicotine patches for helping smokers to stop smoking for one year at least.

REFERENCES:

Ellenhorn’s Medical Toxicology, 1997.

http://news.bbc.co.uk/hi/arabic/news/newsid809000/809287.stm      

 


DOXOFYLLINE:
 A NEW GENERATION XANTHINE BRONCHODILATOR

 

     Doxofylline [7 - (1,3 - dioxalan – 2 -ylmethyl) theophylline] is a novel xanthine bronchodilator which differ from theophylline in that it contains a dioxalane group in position 7. Similar to theophylline, its mechanism of action is related to inhibition of phosphodiesterase activities, but in contrast it appears to have decreased affinities towards adenosine A1 and A2 receptors, which may account for its better safety profile.

     It is well known that cardiac rhythm disturbances are frequent findings in patients with chronic bronchitis and emphysema. The pathogenesis of arrhythmia is complex and many factors may be involved, such as hypoxaemia, hypercapnia, respiratory acidosis, hypokalemia, and concomitant ischemic heart disease.
       Over the years, much attention has been drawn to possible arrythmogenic effects of drugs such as theophylline, B- adrenergic agonists and digitalis, all of which are commonly used in the treatment of chronic obstructive pulmonary disease (COPD). These drugs may become hazardous because of direct stimulatory effects, and therefore, should be used with caution.
        The bronchodilating activities of doxofylline have been demonstrated in clinical trials involving patients with either bronchial asthma or COPD. In contrast to other bronchodilators, experimental and clinical studies have shown that the drug is devoid of direct stimulatory effects. This may be of importance because the arrythmogenic action of bronchodilators may have a negative impact on the survival of patients with respiratory diseases.

In patients with acute respiratory syndromes (acute asthma or exacerbation of COPD), the administration of doxofylline (a bolus of 5 mg/kg followed by an 0.6mg/kg hourly infusion for 24 hours) was associated with a progressive decrease in the heart rate that paralleledβthe clinical improvement. The unique cardiovascular tolerability profile of doxofylline makes it unnecessary to monitor the serum levels of the drug. This is also the reason why in clinical studies it was not necessary to measure extensively the serum level of the drug for the determination of the upper limit of its therapeutic range. To date, the monitoring of the circulating concentration of doxofylline is recommended only in cases of severely impaired hepatic clearance or in the presence of concomitant therapies with quinolones.

REFERANCE:

http://www.medscape.com/librapharma/CMRO/2000/v16.no4/cmr1604.05.dini/cmr1604.05.dini-01.html

 


KOLA NUT IS LIFE

 

     Kola is fruit of cola acuminata, an evergreen tree up to about 20 m high, native to Western Africa with long leathery leaves, and pods containing one to several fleshy and rosy seeds with more than two cotyledons each.

     The part used is the dried seed from which the seed coat has been removed. Dried kola contains caffeine, theobromine, tannins and phenolics including d-catechin. L-epicatechin, kolatin. Also contains phlobabaphene, anthocyanin, pigment kola red, betaine, protein and starch. All of these substances are completely natural and most exist only when the nut is fresh.

     The medicinal uses through out history include:

 *increasing the capacity for physical exertion and for enduring fatigue without food.

 *stimulating a week heart   *impotence..

 *treating nervous debility.  *weakness.

 *lack of emotion.                *depression.

 *nervous diarrhea.              *migraine.

 *sea sickness.                     *anxiety.                      

     Scientists are not completely sure how the nut does its magic, but it is theorized that the mixture of agents in the nut work together to increase blood flow, create euphoric state, and generally increase the desire to have sex. Statements from women who have tried the nut have even indicated positive results from them.

REFERANCES:

http://216.142.243.171/africanwood/

http://homeget,net/karcher//stories/kolanut.htm

http://www.natra-group.com/kolanut.hml

 


VENOM FROM MARINE SNAILS FIGHTS AGAINST CANCER PAIN

 

     Ziconotide, a chemical component derived from the venom of predatory core snails, which stab and paralyze passing fishes before eating them, has been found to relieve severe pain in cancer patients.

     Ziconotide is an analgesic rather than an anesthetic, so it relieves pain without numbing the affected area.

 The authors tested ziconotide in a double-blind, placebo-controlled trial on 108 patients with cancer who had severe chronic pain. They administered ziconotide through a catheter, which dripped the drug slowly into the patients’ spinal fluid. Upon analysis of the drug trial data, the researchers found that ziconotide was highly effective in relieving pain. Pain relief did not vary depending on the age or sex of the patient. Ziconotide also worked equally well regardless of whether the patient had previously been treated with morphine.

The researchers have observed that ziconotide seems to be effective in treating pain from nerve injuries as well as cancer pain. They also think that it might be a good neuroprotective agent for people undergoing heart-lung bypass. This promises to be the first of a whole new class of pain drug that may be able to treat people resistant to other types of drugs.

REFERENCE:

http://pharmacistsmedscape.com/medscapewire/2001/05/medwire.0516.venom.html


الإقلاع عن التدخين باستخدام عقار زيبان

أعلن العلماء البريطانيين عن عقار جديد يساعد علي الإقلاع عن التدخين وهو عقار الزيبان (بيبروبيون هيدروكلوريد).  ويعتبر الزيبان من الأدوية المضادة للاكتئاب وليس له علاقة بالأدوية المضادة للاكتئاب الثلاثية الحلقة أو الرباعية الحلقة أو بالأدوية التي تقوم بإيقاف تكسير السيروتونين وطريقة عمله تعتبر غير واضحة حتى الآن. الإدمان علي النيكوتين قد يكون في شدة الإدمان علي أقوي المخدرات كالهيروين والكوكايين وخلال عشر ثواني فقط من استنشاق الدخان من السيجارة حيث تدخل جرعة من النيكوتين مباشرة وبسرعة إلي المخ مما يؤدى إلى إفراز الدوبامين والنورأدرينالين وعندما يقلع المدخن عن التدخين فإن مستوي هذه المواد يتغير وهذا بدوره يؤدى إلي الإحساس بالحاجة إلي النيكوتين وزيادة القلق والتوتر. وما يفعله الدواء الجديد هو تدخله في عملية الإدمان ذاتها وذلك عن طريق إبقاء مستوي تلك المواد في المخ علي ما كانت عليه قبل الإقلاع. وقد أظهرت دراسة نشرت في أحد المجلات العلمية أن30,3% من المدخنين الذين عولجوا بأقراص زيبان أصبحوا غير مدخنين خلال عام.


دوكسيفيللين عقار جديد موسع للشعب الهوائية

يعتبر دوكسيفيللين من العقاقير الجديدة الموسعة للشعب الهوائية ويختلف عن عقار الثيوفيللين في احتواء الأول علي مجموعة دايوكسيلين في المركز رقم 7 وبالرغم من أن طريقة عمله لا تختلف عن عقار الثيوفيللين في تثبيط إنزيم الفوسفودايستيريز إلا أن درجة رغبته تجاه مستقبلات الأدينوزين أ1 ، أ2 تكون أقل من عقار الثيوفيللين وهذا يجعله أفضل من موسعات الشعب الهوائية  الأخرى في أن تأثيره علي القلب أقل ولذلك فإن الأطباء يستخدمون هذا العقار في مرضي القلب وبدون الحاجة الدائمة لقياس مستوي العقار في الدم  ويلجأ الأطباء لهذا القياس عند استخدام هذا العقار مع مرضي الكبد أو عند استخدامه في نفس الوقت مع عقار من مجموعة الكينولين. 

 


جوزة الكولا (القورو) هي الحياة

جوزة الكولا (القورو)  ثمرة تنبت في وسط أفريقيا والأجزاء المستعملة فيها هي البذور حيث تحتوى علي الكافيين والثيوبروميين والتانين ومكونات أخرى فينولية ولها استخدامات طبية عديدة منها علاج حالات الضعف العام والضعف الجنسي والاكتئاب والإسهال العصبي ودوار البحر وكمنشط للقلب.  


سم القواقع البحرية يقضي على آلام السرطان

تم استخراج مادة كيميائية تسمى زيكوناتايد من سم بعض القواقع المفترسة وقد وجد أن هذه المادة تخفف الآلام الشديدة لمرضى السرطان بدون أي تأثير مخدر وقد تبين من الدراسة التي تضمنت عدد 108 من مرضى السرطان الذين أعطوا مادة الزيكوناتايد ببطيء عن طريق قسطرة داخل السائل الشوكي أن هذه المادة فعالة جداً في تخفيف الألم ووجد أن تخفيف الألم لا يختلف من مريض لآخر مهما اختلف العمر أو الجنس وكذلك مهما تعاطي المريض مورفين من قبل أم لا.