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Posts Tagged ‘COX’

A-Z Principal Drugs (nisoldipine - oxerutins)

Saturday, June 27th, 2009

nisoldipine A calcium channel blocking agent of the nifedipine type. Used in mild to moderate hypertension pertension and in the prophylaxis of chronic angina.
Dose: 10 ing once daily before breakfast with adequate fluid, slowly increased as required up to 40 mg daily. Tablets to be swallowed whole, not chewed or crushed. It may react with sonic other drugs in common use, and grapefruit juice should be avoided. (Syscor). See pages 114 & 148, and ‘Fables 4 & 21.
nitrazepam A benzodiazepine used as a mild hypnotic when some degree of daytime sedation is acceptable.
Dose: 5-10 mg at night, with reduced doses for elderly patients, and in renal and’ hepatic dysfunction. Care is necessary in respiratory depression. Some dependence on nitrazepam may occur, so extended treatment should be avoided. The combined use of alcohol increases the hypnotic action. (Mogadon; Remnos). Set: page 152 and Table 22.
Nitrocine A solution of glyceryl trinitrate, for i.v. infusion in myocardial ischaemia and refractory angina.
nitrofurantoin An antibacterial agent with a wide range of activity against the majority of urinary pathogens. It is of value in cystitis and pyelitis, and in renal infections that have become resistant to other drugs. It is also used prophylactically but extended use requires care.
Dose: 400 mg daily; 50-100 mg at night for prophylaxis. It is ineffective in an alkaline urine. Nausea, rash and peripheral neuropathy are side-effects, and acute and chronic pulmonary reactions have been reported. (Furadantin; Macrobid).
nitroglycerine See glyceryl trinitrate. nitroprusside See sodium nitroprusside.
nitrous oxide The oldest inhalation anaesthetic. Supplied in blue cylinders, it is widely used for induction and as part of a mixed anaesthetic system. It is also used as
a 50% oxygen mixture as an inhalation analgesic in obstetrics.
nizatidine A potent and selective H,-receptor antagonist chemically distinct from cimetidine or ranitidine.
Dose: in the treatment of benign duodenal and gastric ulcer, single doses of 300 mg daily, taken in the evening, or 150 mg twice a day, and continued for 4 weeks, or for s weeks in gastric ulcer including non-steroidal anti-inflammatory agent (NSAID) -induced ulceration. Occasionally given by i.v. infusion in doses of300mg daily. For prophylactic maintenance, doses of 150 mg daily may be given for up to a year. Reduced doses should be given in renal impairment. Side-effects include headache, niyalgia, cough, pruritus and abnormal dreams. (Axi& Zinga). See page 162 and “Fable 27.
non-steroidal anti-inflammatory drugs (NSAIDs) A group of drugs with analgesic anti-inflammatory properties widely used in arthritic, rheumatoid and related conditions. The response to a NSAID and the incidence and severity of side-effects such as gastric irritation and renal toxicity vary considerably, and the best NSAID for an individual patient is the one that gives optimum relief with minimal side-effects. The NSAIDs, of which aspirin is the oldest example, act by interrupting the biosynthesis of prostaglandins from arachidonic acid, in which process the enzyme cycleoxygenase (COX) plays a key role. It is now known that COX exists in two forms identified as COX-1 and COX-2. The anti-inflammatory action of the NSAIDs appears to be linked with the inhibition of COX-2, whereas the unwanted side-effects are associated with COX- I inhibition. Different NSAIDs have varying degrees of activity against the different forms of COX, which may explain the differences in the therapeutic response and the incidence of side-effects. Recently, a NSAID (meloxicain) has been introduced that has a more selective inhibitory action on COX-2, with which the incidence of side-effects appears to be lower than with the older drugs, and so may have therapeutic advantages. In general, the response to a NSAID may take 1-3 weeks to develop fully, but monitoring for gastrointestinal bleeding may be advisable if treatment is extended. A NSAID should not be given to a patient with a history of asthma or hypersensitivity, nor when peptic ulcer is suspected or present. In all cases, treatment should be commenced with the lowest recommended dose, and caution is necessary in the elderly, and when renal or hepatic function is impaired. See page 165 and Table 29.
Dose: 20 100 mg daily. It is given in nocturnal enuresis in doses of 10-20 mg nightly, but the duration of treatment should not exceed 3 months. (Allcgron). See page 128 and Table 11.
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noradrenaline (norepinephrine) The pressor hormone released at sympathetic nerve endings when such nerves are stimulated. It is also present with adrenaline in the medulla of the adrenal gland. It raises blood pressure mainly by a general vasoconstriction, whereas adrenaline acts by constricting the peripheral vessels and increasing the cardiac output. Noradrenaline is given by slow i.v. infusion in the treatment of shock, peripheral failure, and low blood pressure states, but the response may fluctuate with small variations in dose. The value of vasoconstrictors in shock is now questioned, as in shock the peripheral resistance may well be high, and the blood supply to essential organs such as the kidneys may be reduced.
Dose: 2-20 pg/niin, based on need and response. Great care must be taken to avoid extra-venous injection. (Levophed).
norethisterone An orally active progestogen. Used in amenorrhoea, functional uterine bleeding and dysmenorrhoea. Dose: 5-20 mg daily. In breast cancer, large doses up to 60 mg daily have been used. To postpone menstruation, 15 mg daily for 3 days have been used. In small doses, and in association with an oestrogen, norethisterone and related drugs are widely used as oral contraceptives. See page 264.
norfloxacin A quinolone antibacterial with the actions, uses and side-effects of cinoxacin and other quinolones.
Dose: in acute urinary tract infections, 801) mg daily for 3-10 days: in chronic infections continued for up to 12 weeks. ( I Itinor).
norgestrel (levonorgestrel) An orally active progesterone-like drug and inhibitor of ovulation. Used as a constituent of mixed oral contraceptive products, and as a ‘progestogen -only’ oral contraceptive. See page 264.
nortriptyline A tricyclic antidepressant with actions, uses and side-effects similar to those of amitriptyline, but with a reduced sedative activity.
NSAIDs See non-steroidal anti-inflamma-
tory drugs, page 168 and Table 29.
nystatin A fungicidal antibiotic, used in the treatment of intestinal, vaginal and superficial candidiasis. Oral tablets contain 500 000 units, pessaries contain 100 000 units; cream and ointment 1%. Dose: (oral) 2 million units daily. It is also used as pastilles of 100000 units for mouth infections.
octreotide A synthetic compound that inhibits the release of the growth hormone. It is used in acromegaly, which is caused by an overproduction of the growth hormone by a pituitary tumour and it is given in doses of 100-200pg 8-hourly by s.c. injection. It is also used in the symptomatic treatment of the carcinoid syndrome, in which the release of vasoactive substances by a gastro- pancreatic tumour causes flushing and severe diarrhoea.
Dose: 30 pg by s.c. injection, increased as needed up to 600 pg daily. It has no action on the cause of the syndrome. It is used occasionally in terminal care to reduce intestinal secretions and vomiting. Dose: 300-600 pg by s.c. infusion. (Sandostatin).
oestradloIlThe oestrogenic hormone controlling ovulation and menstruation. It has been used to control menopausal symptoms in doses of 10-20pg daily, but skin patches are now preferred for hormone replacement therapy (HRT). It is used occasionally as s.c. implants for long-term treatment. Oestradiol is also present in some cream preparations for menopausal atrophic vaginitis.
oestriol A natural oestrogen used in intravaginal cream to relieve the atrophic vaginitis and kraurosis vulvae associated with the menopause. Also given in doses of 1-32 mg daily for the genito-urinary symptoms linked with infections in oestrogen deficiency states. (Ovestin).

ofloxacin A fluorinated quinolone with the actions, uses and side-effects of other quinolones such as ciprofloxacin and norfloxacin. It is used mainly in urinary and lower respiratory tract infections. Dose: wii nig daily as a single morning dose. Dose in severe infections 200-400 mg daily by i.v. injection. An occasional side-effect is tendon damage with pain and inflammation, which requires immediate withdrawal of the drug. Exposure to strong sunlight should be avoided. (Tarivid). Also used as eye drops (0.3%) for superficial eye infections. (Exocin).
olanzapineV An antipsychotic agent for the treatment of schizophrenia. It has a more selective action on certain 5-H’I'- receptors, and is less likely to cause extra-pyramidal side-effects.
Dose: 10 mg as a single daily dose, slowly increased as required. Maintenance dose 5-20 mg daily. Side-effects include
sedation and weight gain. (Zyprexa). See page 168 and Table 30.
olsalazine A compound formed from mesalazine, and used in the treatment of ulcerative colitis. It is more slowly
absorbed, and reaches the colon largely unchanged, where it is broken down by intestinal bacteria to release the active metabolite mesalazine.
Dose: 1-3 g daily in acute mild ulcerative colitis; I g daily for maintenance, often for long periods. The common side-effect is a watery diarrhoea. Salicylate sensitivity is a contraindication. Patients are now advised to report any bruising, bleeding or
malaise. I( a blood dyscrasia is suspected, a blood count should be made -,in(] the drug withdrawn. (Dipentuni). See page 172 and Table 32.
ondansetron A potent antiemetic, of value in the nausea and vomiting associated with cancer chemotherapy. Such vomiting appears to be induced by the release of serotonin, which acts on receptors in the gut as well as stimulating the chernoreceptor trigger zone in the brain. Ondansetron is a specific (5—HT,) serotonin blocking agent, and is given before the commencement of cytotoxic treatment or radiotherapy.
Dose: 24 mg daily; in severe vomiting an initial dose of 8 ing is given by slow i.v. injection, followed by I ing/hrly for 24 hours by continuous i.v. infusion, followed by oral therapy. Side-effects are an initial sense of warmth, headache an(] constipation. (Zofran). See page 158.
topium The dried juice from the capsules of the opium poppy. See morphine.
orciprenaline A synipathomimetic agent with the bronchodilator properties of isoprenaline. It is used for the relief of obstructive airway conditions, although more selective drugs of the salbutarnol type are often preferred.
Dose: up to 80 ang daily; by aerosol inhalation up to 12 puffs (9mg) daily. Side-effects include tremor and tachycardia. (Ahiperil). See page 118 and Table 6.
orphenadrine A spasmolytic drug, used in the treatment of parkinsonism, and for the relief of voluntary muscle spasm. Dose: 150-400 nig daily. It may also be given by i.m. injection in doses of 60 mg. In parkinsonism it tends to control the rigidity more than the tremor. Side-effects are anticholinergic and include dryness of the mouth, dizziness and visual disturbances. Weight gain has occurred with high doses. (Disipal; Norflex). See
page 160 and Table 26.
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omeprazole An inhibitor of the enzyme I I*K’A'I’Pase.’rhat enzyme controls the final stage of gastric acid production, and its inhibition by omeprazole is of value in peptic ulcer resistant to H, receptor antagonists, and in reflux oesophagitis, where such agents are not always effective. Dose: in benign gastric and duodenal ulcer, 20-40 ing as it single daily dose for 4-8 weeks. Larger doses may be required in the Zollinger—Ellison syndrome. Side-effects such as nausea, gasiro-intestinal disturbances and headaches are usually mild. (Losec). See page 162 and Table 27.
oxazepam A benzodiazepine with the actions, uses and side-effects of diazepam. It is useful in acute anxiety and panic states.
Dose: 45-120 mg daily. See page 117 and Table 5.
oxerutins A mixture of rutosides (flavonoid derivatives) which is claimed to reduce capillary fragility and permeability. It has been used in venous disorders of the lower limbs.
Dose: 750-1000 nig daily. (Paroven).