Thursday, July 30th, 2009
Bisphosphonates (bis-FOS-fun-ates)
Brand Names
Alendronate Sodium Fosamax
Alendronate Sodium Cholecalciferol Fosamax Plus D
Etidronate Disodium (9 Didronel
lbandronate Sodium Boniva
Risedronate Sodium 91 Ar.Wm~
Risedronate Sodium Calcium Carbonate Actonel with Calcium
Tiludronate Disodium Skelid
Prescribed For
Prevention and treatment of osteoporosis (a condition characterized by loss of bone mass due to calcium depletion) in postmenopausal women and in older men; Paget’s disease of bone; and high blood calcium associated with high dosages of corticosteroid treatments and cancer.
General Information
Bisphosphonates have been used for many years to treat a variety of conditions associated with low bone mass caused by calcium depletion. They work on cells called osteoclasts that normally break down bone tissue, making bones stronger by preventing loss of bone mass. In osteoporosis, bones become weak and brittle, increasing the risk of spine, hip, and other bone fractures that are a major cause of death and disability in older women. Etidronate has been used occasionally in children, but these drugs generally are not considered safe for use in children.
Cautions and Warnings
Do not use any bisphosphonate if you are allergic or sensitive to any of its ingredients.
Do not use bisphosphonates if you have severe kidney disease or active stomach or intestinal disease such as difficulty swallowing, ulcers, or stomach irritation. Notify your doctor if you experience any gastrointestinal problems while taking bisphosphonates.
Osteonecrosis of the jaw (ONJ), a condition in which bones of the jaw lose their blood supply and eventually collapse, has been reported in people treated with bisphosphonates. Most cases of ONJ have been in cancer patients having dental procedures such as tooth extractions. People at risk may be those with cancer and those taking corticosteroids or those with poor oral hygiene.
Do not use ibandronate, alendronate, or risedronate it you cannot stand or sit upright for 30 minutes (see “Special Information”).
Bisphosphonates can cause low blood calcium and should not be used by people whose blood calcium is already low.
Bisphosphonates can cause severe and sometimes incapaciating bone, muscle pain.
Possible Side Effects
Side effects are generally mild and similar to those reported by people taking an inactive placebo (sugar pill).
Possible Side Effects (continued)
Alendronate
♦ Most common: pain.
✓ Common: abdominal pain and discomfort, gas, stomach ulcers, and back pain.
✓ Less common: upset stomach, constipation, diarrhea, nausea, difficulty swallowing, muscle pain, headache, flu-like symptoms, accidents, and swelling in the arms or legs.
♦ Rare: vomiting and changes in taste. Contact your doctor it you experience any side effect not listed above.
Etidronate
✓ Most common: fever.
✓ Common: nausea, excess fluids, and flu-like symptoms.
♦ Less common: convulsions, constipation, inflammation of the lining of the mouth, changes in liver function, low blood levels of magnesium or phosphate, breathing difficulties, and changes in sense of taste.
✓ Rare: allergic reactions. Contact your doctor if you experience any side effect not listed above.
lbandronate
✓ Most common: upper respiratory infection, back pain, bronchitis, and upset stomach.
♦ Common: arm or leg pain, muscle pain, headache, pneumonia, and urinary infections.
✓ Less common: dizziness, fainting, pain due to nerve lesions, weakness, allergic reactions, diarrhea, vomiting, dental problems, stomach pain, low blood cholesterol, joint problems, arthritis, and sore throat.
✓ Rare: eye problems have occurred with other drugs in this group but not with ibandronate. Contact your doctor if you experience any side effect not listed above.
Risedronate
✓ Most common: qlaftea, abdominal pain, rash, and severe joint pain.
✓ Common: chest pain, dizziness, swelling in the arms or legs, constipation, nausea, sinus irritation, and bone pain.
✓ Less common: leg cramps, weakness, bronchitis, poor vision in one eye, dry eyes, ringing or buzzing in the ears, Possible Side Effects (continued)
parathyroid gland problems, infection, rash and other skin problems, tooth problems, and vitamin D deficiency.
♦ Rare: fatigue and drug reactions, including swelling of the
tongue and throat with difficulty breathing, generalized rash,
and some blisters. Contact your doctor if you experience
any side effect not listed above.
Tiludronate
♦ Most common: diarrhea and nausea.
✓ Common: headache, upset stomach, respiratory infection, runny nose, fluid in the lungs, and sinus irritation.
✓ Less common: vomiting, dizziness, tingling in the hands or feet, coughing, sore throat, gas, aches and pains, cataracts, eye redness, glaucoma, rash, skin disorders, tooth problems, swelling, infection, vitamin D deficiency, and muscle aches.
♦ Rare: tiredness, high blood pressure, fainting, appetite loss, constipation, abdominal pain, and sleeplessness. Contact your doctor if you experience any side effect not listed above.
Drug Interactions
• Antacids, calcium, and iron-containing supplements and foods can interfere with the absorption of bisphosphonates. Separate doses of these drugs and foods and a bisphosphonate by at least 30 minutes.
• Separate doses of tiludronate and aluminum-containing antacids by 1 hour.
• Aspirin can interfere with the absorption of tiludronate.
• Indomethacin can increase the amount of tiludronate absorbed into the blood by 2-4 times.
• Bisphosphonates may increase the gastrointestinal-irritating effects of aspirin, ibuprofen, and other NSAWDs.
• Drugs that reduce the amount of stomach acid, including ranitidine, cimetidine, and omeprazole, may increase the amount of ibandronate in the blood, but the degree of increase is not clinically important.
• Etidronate may affect the action of warfarin.
• Bisphosphonates reduce the ability of teriparatide to build new bone.
Food Interactions
Take these medicines with plain water. Food and drink—even mineral water, orange juice, or coffee—interfere with the absorption of these drugs. Take alendronate or risedronate every morning at least 30 minutes before eating, drinking, or taking other medications. Etidronate should be taken on an empty stomach 2 hours before a meal. lbandronate should be taken as soon as you wake up and 1 hour before you eat or take any other medications, vitamins, or supplements. Tiludronate should be taken when you first wake up; wait 4 hours before eating breakfast.
Usual Dose
Alendronate
10-40 mg a day; or 35-75 mg once weekly. not recommended.
Alendronate + Calcium
70 mg/2800 IU once weekly. not recommended.
Etidronate
up to 4.5 mg per lb. a day to start, gradually increasing to no more than 9 mg per lb. per day.
not recommended.
lbandronate
2.5 mg.once a day: or one 150 mg tablet once a month. not recommended.
Risedronate
5-30 mg a day; or 35 mg once weekly. not recommended.
Tiludronate
400 mg a day.
not recommended.
Overdosage
Little is known about the effeckS,zA USP*nosphonate overdose.
Other symptoms include upset stomach, heartburn, ulcer, and irritation of the esophagus. Milk or antacids may reverse these effects. These drugs can irritate the esophagus. Do not let the victim lie down or vomit. Overdose victims should be taken to a hospital emergency room. ALWAYS bring the prescription bottle or container.
Special Information
Food interferes with the effectiveness of these drugs. Carefully follow the directions in “Food Interactions” above.
Do not suck on any of these tablets or allow them to dissolve in your mouth because they can cause mouth sores.
To reduce the risk of stomach and throat irritation, do not lie down for at least 30 minutes after taking alendronate or risedronate. Do not lie down for 60 minutes after taking ibandronate.
Separate doses of calcium, iron, and vitamin D supplements from those of a bisphosphonate by at least 2 hours. If you forget a dose, take it as soon as you remember. If it is almost time for your next dose, skip the dose you forgot and continue with your regular schedule. If you forget a morning dose and take it later in the day, you must still follow the instructions in “Food Interactions” about avoiding food.
Special Populations
Pregnancy/Breast-feeding: Bisphosphonates cause abnormal bone development in animal fetuses and are toxic to pregnant animals. When any of these drugs is considered crucial by your doctor, its potential benefits must be carefully weighed against its risks.
It is not known if bisphosphonates pass into breast milk. Since these drugs affect bone formation, nursing mothers who must take a bisphosphonate should use infant formula.
Seniors: Seniors may use these drugs without special restriction.
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Friday, June 26th, 2009
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ethinyloestradiol A synthetic oestrogen formerly used to control menopausal symptoms and other conditions where oestrogen therapy is indicated.
Dose: 10-50 pg daily. It is present with a pi ugestogen in many oral contraceptive products. See page 264 and Table 40.
othosuximide An anticonvulsant for the treatment of petit trial epilepsy (absence seizures). May be used alone, or combined with other anticonvulsants, and it is often of value in patients not responding to other drugs.
Dose: 500 nig daily initially, gradually increased if required, to a maximum of 2 g daily. Care is necessary in renal or hepatic disease. Drowsiness, headache and gastrointestinal disorders are sonic side-effects. (F meside; Zaronlin). See page 136 and Table 15.
etidronate disodium A bisphosphonate used in Paget’s disease of bone, as it slows down the rapid turnover of bone and relieves the pain of that disease.
Dose: 5 nig/kg as a single daily dose between meals for 6 months or more. Side-effects are nausea and diarrhoea; high (loses may increase bone pain and the risks of fracture. (Didronel). Didronel PMO also contains calcium carbonate, and is used in the extended treatment of vertebral osteoporosis. See clodronate and pamidronate.
include nausea, alopecia and myelosuppression. (Vespid). See page 122 and Table 8.
eusol A chlorine antiseptic solution used as lotion, or as compress. The solution should be freshly prepared. Now less popular, thought to be irritant.
evening primrose oil See gamolenic acid.
eye drops Weak solutions of drugs for the treatment of ocular conditions. They may be antibacterial, antifungal or antiviral in action, or maybe used for non-infective conditions such as glaucoma, or for diagnosis. For routine use they are supplied sterile in multiple-application containers, but are intended for individual use only. They contain preservatives, and for home use may be used for up to one month after the container has been opened. In eye Surgery, single application products should be used. Occasionally, enough of a drug may be absorbed from eye drops to have systemic effects, and corticosteroids, if used as eye drops over a prolonged period, may cause’steroid glaucoma’. Care should be taken with contact lenses, and ideally they Should not be worn during eye drop treatment. Soft contact lenses can absorb the preservatives, which may cause irritation.
etodolac A non-steroidal anti-inflammatory agent (NSAID) of the naproxen type, with similar actions, uses and side-effects. Dose: in rheumatoid conditions, 400 mg daily. (Lodine). See page 169 and
Table 29.
etomidate A short-acting i.v. hypnotic used lor the induction of anaesthesia. It causes little cardiac disturbance or hypertension, but muscle movement and pain may
occur during injection.
Dose: 300 pg/kg by i.v. injection.
f Ilypnomidate).
etoposide A cytotoxic agent used in small-cell lung cancer and resistant testicular cancers. It is given in daily doses based on skin area for 5 days, repeated after 21 days according to response.
Dose: 120-240 nighn’ daily orally; by i.v. infusion 60-120 mghn’, and care must be taken to avoid extravasation. Side-effect-,
Factor Vila A recombinant and active form of the blood coagulation Factor VII. The treatment of haemophilia with Factors Vill and IX is complicated by the development of antibodies to those factors. Factor Vila acts as a late stage in the conversion of fibrinogen to fibrin, can function independently of Factors Vill and IX, and does not induce the formation of antibodies. It is used to control serious bleeding in haemophiliac patients and during surgery, under specialist supervision.
Dose: 60-120pg initially by i.v. injection, followed by a second dose after 2-3 hours, then 4-12-hourly as required for
2-3 weeks or more. (NovoSeven).
Factor Vill Haemophilia A is caused by a deficiency of the blood clotting agent Factor Vill, and highly purified preparations of human Factor VIII as well as recombinant forms are used as replacement therapy in doses based on the degree of deficiency of that factor. (Kogenate; Monoclate P; Recombinate).
Factor IX Haemophilia B is due to a deficiency of Factor IX, and preparations of that factor, obtained by monoclonal antibody techniques, are given i.v. in doses based on the degree of efficiency of the factor. (Monomine; Replenine).
famiclovir An antiviral agent similar to acyclovir, and used in herpes zoster (shingles) and genital herpes infections. Dose: 75 mg daily for 7 days. (Panivir). See page 144 and “fable 19.
famotidine An H,-receptor antagonist with the uses and side-effects of cinictidine, but a longer action.
Dose: in benign peptic ulcer, 40 ing at night lor,1-8 weeks; 20 mg at night for the prevention of recurrence, also used in reflex oesophagitis. In Zollinger-Ellison
syndrome, doses of 20 mg 6-hourly are given. ( Pepcid). See page 162 and] *able 27.
pain and inflammation in rheumatoid arthritis and similar conditions.
Dose: 600-900 nig daily. Like other
NSAIDs, it may cause gastrointestinal disturbance and dizziness, but the incidence of rash requires withdrawal of the drug. (Leclet-fen). See page 165;uidfable 29.
fencifibrate A plasma-lipid regulating agent of the clofibrate type, with similar uses and side-effects.
Dose: 300 ing initial]),, with food, later 200-400 mg daily according to need. (Lipantil). See page 146 and Table 20.
fenoprofen A non-steroidal anti-inflammatory and anti-rheumatic agent. It is also used as a mild analgesic in a variety of painful conditions.
Dose: 900 mg-3 g daily. Side-effects include nausea, dizziness, vertigo and rash. (Fenoprofen; Progesic). See page 165 and Table 29.
fenoterol A sympathomimetic agent with the actions, uses and side-effects of salbutamol. Dose: by oral inhalation, 100-200 [Ig (1-2 puffs) up to 4 times a day. (Berotec). See page 118 and Table 6.
Fansidar Pyriniethamine, 25 mg with sulfadoxine 500 mg. Both these antimalarial drugs block the formation of folinic acid in the malarial parasite, but the combination is more effective. Mainly used with quinine in resistant filciparum malaria. (Fansidar is no longer recommended for prophylaxis, as fatalities have followed such use.)
felodipine A calcium antagonist used in the treatment of hypertension generally (see calcium channel blocking agents). Dose: 5 nig daily initially, adjusted to maintenance doses up to to mg daily. ‘I abiets should be taken in the morning, and swallowed whole with water. No adjustment of dose necessary for elderly patients, but care is required in marked hepatic impairment. Hypotension with tachycardia may occur with susceptible patients. (Plendil). See page 148 and Table 21.
felypressin A vasopressin derivative, used as a vasoconstrictor in local anaesthetic solutions for dental use, when sympathetic pressor drugs are contraindicated.
fenbufen A non-steroidal anti-inflammatory agent (NSAID) used for the relief of
fentanyl A narcotic analgesic, used mainly in thiopentone anaesthesia to increase the response and permit a reduction in dose of thiopentone, especially in poor-risk patients. It is also used with droperidol to produce a state of neuroleptanalgesia. Dose: 50-200 pg by i.v. injection.
(Subli niaze). Also used as a patch for the relief of chronic pain. (Durogesic).
fenticonazole An antifungal used in vaginal candidiasis as pessaries of 200 mg. (Lonlexin).
ferrous sulphate, fumarate, gluconate & succinate These iron salts are used in the prophylaxis and treatment of iron-deficiency anaemias. Ferrous sulphate is the standard drug, given in doses of 600 mg daily, but it may cause gastric disturbance in some patients, and ferrous fumarate, gluconate and succinate are better tolerated alternatives. Sonic better tolerated slow-release products are available, but may be less well absorbed. Ferrous sulphate tablets are potentially dangerous for small children, and death has occurred after accidental administration. See desferrioxamine.
fexofenadine An antihistamine with the general properties of that group of drugs. It is less likely to affect the ability to drive. Dose: 120 mg once daily. See
page 110 and Table 2.
fibrinolytic agents Drugs used to break up blood clots, and so are of value in thrombosis. See alteplase, anistreplase, streptokinase and urokinase.
filgrastim A recombinant form of human granulocyte colony stimulating factor (G-CSF), one of a group of natural growth factors concerned with bone marrow activity. It stimulates the development of neutrophils, the production of which is depressed during cytotoxic therapy. The neutropenia thus caused increases the risks of infection, but the neutrophil count can be restored by filgrastim. It is used mainly in the neutropenia associated with the cytotoxic treatment of non-myeloid malignancy. Dose: 500 000 units/kg daily by s.c. injection or i.v. infusion for 14 days, or until the neutrophil count return, to normal. Double doses are given after bone marrow transplanlation.The main side-effects are musculoskeletal pain and dysuria. See lenograstini and molgrastirn.
His, and is of value in serious ventricular tachycardia and extrasystoles.
Dose: 200-400 mg daily. May he given by slow i.v. injection in doses of 2 iiig/kg in acute conditions resistant to other therapy, and under hospital control. Care is necessary in patients with pacemakers, and in renal impairment. Dizziness and visual disturbances are side-effects. (Tainhocor). See page 141 and Table 18.
flucloxacillin A derivative of cloxacillin, that is absorbed more readily when given orally. It is used mainly in infections due to penicillinase-producing penicillin-resistant staphylococci.
Dose: I g daily before food; by injection 1 -4 g daily, but larger doses arc given in very severe infections. Side-effects are those of the penicillins generally. (Floxapen). See co-fluanipicil.
fluconazole A systemically acting synthetic antifungal agent.
Dose: in oral candidiasis, 50 ing daily for 7-14 days: in vaginal candidiasis, a single dose of 1.50 mg. Dose in systemic candidiasis and cryptococcosis, 200-400 mg daily orally or by i.v. infusion. Side-effects include nausea and abdominal discomfort. Combined treatment with
asternizole, cisapride or terfenadine should be avoided. (Dillucan).
finasteride An inhibitor of the enzyme 5-alpha reductase, and so prevents the conversion of testosterone to dihydrotestosterone, the biologically active form of the male hormone. It is used for the symptomatic relief of benign prostatic hyperplasia, as prolonged therapy promotes a reduction in the size of the prostate gland.
Dose: 5 nig daily for 6 months or more. Side-elfects are reduced libido and impotence. (Proscar). See page 164 and Table 28.
flavoxate An antispasmodic of value in urinary disorders such as dysuria, frequency and related conditions. Dose: 600 mg daily. Side-effects include dry mouth and blurred vision. Contraindicated in glaucoma and bladder obstruction. (Urispas).
flecainicle An orally active anti-arrhythmic
agent of the lignocaine type. It chiefly
influences conduction in the bundle of
flucytosine An antifungal agent used in systemic yeast infections such as candidiasis and cryptococcosis.
Dose: 100-200 mg/kg daily i.v. It may Cause sonic bone marrow depression, and sensitivity tests should be carried out before and during treatment, as resistance to the drug may limit its value. Care is necessary in renal and hepatic inipairmclit. Side-effects include nausea, diarrhoea and rash. (Alcobon).
fludarabine A fluorinated cytotoxic agent used in chronic lymphocytic leukaemia (CI.L) after other treatment has failed. Dose by i.v. infusion 25 mg/in’ for 5 days a nionth. It is generally well tolerated, but myclosuppression may occur as with related drugs. (Fludara).
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