Antasida

Omeprazole
For the relief of acid-related dyspepsia omeprazole is given in usual doses of 10 or 20 mg daily orally for 2 to 4 weeks.

The usual dose for the treatment of gastro-oesophageal reflux disease is 20 mg orally once daily for 4 weeks, followed by a further 4 to 8
weeks if not fully healed. In refractory oesophagitis, a dose of 40 mg daily may be used. Maintenance therapy after healing of oesophagitis
is 20 mg once daily, and for acid reflux is 10 mg daily. For dosage in children see below.

In the management of peptic ulcer disease a single daily dose of 20 mg orally, or 40 mg in severe cases, is given. Treatment is continued
for 4 weeks for duodenal ulcer and 8 weeks for gastric ulcer. Where appropriate, a dose of 10 to 20 mg once daily may be given for
maintenance. lin 1 g and clarithromycin 500 mg, both twice daily. These regimens are given for 1 week. Dual therapy regimens such as
omeprazole 20 mg twice daily or 40 mg daily with either amoxicillin 750 mg to 1 g twice daily or clarithromycin 500 mg three times daily,
are less effective and must be given for 2 weeks. Omeprazole alone may be continued for a further 4 to 8 weeks.
For the eradication of Helicobacter pylori in peptic ulceration omeprazole may be combined with antibacterials in dual or triple therapy.
Effective triple therapy regimens include omeprazole 20 mg twice daily or 40 mg once daily combined with: amoxicillin 500 mg and
metronidazole 400 mg, both three times daily; clarithromycin 250 mg and metronidazole 400 mg (or tinidazole 500 mg) both twice daily; or
with amoxiciln

Doses of 20 mg daily orally are used in the treatment of NSAID-associated ulceration; a dose of 20 mg daily may also be used for
prophylaxis in patients with a history of gastroduodenal lesions who require continued NSAID treatment.

The initial recommended dosage for patients with the Zollinger-Ellison syndrome is 60 mg orally once daily, adjusted as required. The
majority of patients are effectively controlled by doses in the range 20 to 120 mg daily, but doses up to 120 mg three times daily have been
used. Daily doses above 80 mg should be given as divided doses (usually 2). Omeprazole is also used for the prophylaxis of acid aspiration
during general anaesthesia, in a dose of 40 mg the evening before surgery and a further 40 mg two to six hours before the procedure
Lansoprazole is usually given orally as capsules, dispersible tablets, or suspension containing enteric-coated granules. Once daily regimens
are taken before food in the morning. An intravenous formulation is also available.

For the relief of acid-related dyspepsia (p.1695) intermittent courses of lansoprazole may be given in doses of 15 or 30 mg once daily, for 2
to 4 weeks.

In the treatment of gastro-oesophageal reflux disease (p.1696) the dose is 15 to 30 mg once daily for 4 to 8 weeks; thereafter maintenance
therapy can be continued with 15 or 30 mg once daily according to response. In patients unable to take oral therapy, lansoprazole may be
given by intravenous infusion for the treatment of erosive oesophagitis for up to 7 days; a dose of 30 mg over 30 minutes daily is
recommended.
Lansoprazole is given for the treatment of peptic ulcer disease (p.1702) in the UK in doses of 30 mg once daily. Treatment is continued for
2 to 4 weeks for duodenal and 4 to 8 weeks for gastric ulcer. In the USA, a dose of 15 mg daily for 4 weeks is recommended for
duodenal ulcer, and 30 mg once daily is given for up to 8 weeks for gastric ulceration. When appropriate, 15 mg daily may be used as
maintenance therapy for the prevention of relapse of duodenal ulcer. Lansoprazole may be combined with antibacterials in one-week triple
therapy regimens for the eradication of Helicobacter pylori. Effective regimens include lansoprazole 30 mg twice daily combined with
clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily, or combined with clarithromycin 250 mg twice daily and metronidazole
400 mg twice daily; lansoprazole with amoxicillin and metronidazole has also been used. In patients with NSAID-associated ulceration a
dose of 30 mg daily for 4 to 8 weeks is recommended; 15 to 30 mg daily may be used as prophylaxis for patients who require continued
NSAID treatment.
In the treatment of pathological hypersecretory states such as the Zollinger-Ellison syndrome (p.1704) the initial dose is 60 mg once daily,
adjusted as required.
Doses of up to 90 mg twice daily have been used. Daily doses greater than 120 mg should be given in divided doses.

Pantoprazole sodium 11.28 mg is equivalent to about 10 mg of pantoprazole. Once-daily doses should be taken in the morning. In the
treatment of gastro-oesophageal reflux disease (p.1696), the usual oral dose is 20 to 40 mg once daily for 4 weeks, increased to 8 weeks if
necessary; in the USA, up to 16 weeks of therapy is permitted for healing of erosive oesophagitis. For maintenance therapy, treatment can be
continued with 20 to 40 mg daily. Alternatively, for recurring symptoms, an on-demand regimen of 20 mg daily may be given. The usual
dose for the treatment of peptic ulcer disease (p.1702) is 40 mg once daily. Treatment is usually
given for 2 to 4 weeks for duodenal ulceration, or 4 to 8 weeks for benign gastric ulceration. For the eradication of Helicobacter pylori
pantoprazole may be combined with two antibacterials in a 1-week triple therapy regimen. Effective regimens include pantoprazole 40 mg
twice daily combined with clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily, or combined with clarithromycin 250 mg
twice daily and metronidazole 400 mg twice daily. Patients who require prophylaxis for NSAID-associated ulceration may take 20 mg
daily.
In the treatment of pathological hypersecretory states such as the Zollinger-Ellison syndrome (p.1704), the initial dose is 80 mg daily,
adjusted as required. Doses of up to 240 mg daily have been used. Daily doses greater than 80 mg should be given in 2 divided doses

Cimetidine
Cimetidine may be given orally, by the nasogastric route, or parenterally by the intravenous or intramuscular routes; the total daily dose by
any route should not normally exceed 2.4 g. Although some formulations are prepared as the hydrochloride, strengths and doses are
expressed in terms of the base. Cimetidine 100 mg is equivalent to about 114.4 mg of cimetidine hydrochloride. Doses should be reduced in
renal impairment and may also need to be reduced in hepatic impairment (see below).
SPECIFIC DISEASE DOSES.
In the management of benign gastric and duodenal ulceration a single daily oral dose of 800 mg at bedtime is recommended, which should
be given for at least 4 weeks in the case of duodenal, and for at least 6 weeks in the case of gastric, ulcers. Where appropriate a maintenance
dose of 400 mg may then be given once daily at bedtime, or twice daily in the morning and at bedtime. Other regimens have also been used
for treatment and maintenance.
In gastro-oesophageal reflux disease the recommended oral dose is 400 mg four times daily (with meals and at bedtime), or 800 mg twice
daily, for 4 to 8 weeks. In pathological hypersecretory conditions, such as the Zollinger-Ellison syndrome, an oral dose of 300 or 400 mg
four times daily is normally used, although sometimes higher doses may be necessary.
Doses of 200 to 400 mg orally, by nasogastric tube, or parenterally (200 mg only for direct intravenous injection) every 4 to 6 hours are
recommended for the management of patients at risk from stress ulceration of the upper gastrointestinal tract. In patients at risk of
developing the acid aspiration syndrome, an oral dose of 400 mg may be given 90 to 120 minutes before the induction of anaesthesia, or at
the start of labour (in obstetric practice), and doses of up to 400 mg (by the parenteral route if appropriate, see below) may be repeated at
intervals of 4 hours if required. Doses of up to 200 mg four times daily have been taken for non-ulcer dyspepsia; 100 mg at night has been
used in the prophylaxis of nocturnal heartburn. To reduce the degradation of pancreatic enzyme supplements, patients with pancreatic
insufficiency, as in cystic fibrosis (p.166), may be given oral cimetidine 800 to 1600 mg daily in 4 divided doses, 60 to 90 minutes before
meals.

Ranitidin
Ranitidine may be given orally or parenterally by the intravenous or intramuscular routes. Although most preparations contain ranitidine
hydrochloride, strengths and doses are expressed in terms of the base. Ranitidine hydrochloride 111.6 mg is equivalent to about 100 mg of
ranitidine.
In the management of benign gastric and duodenal ulceration (p.1702) a single daily oral dose of 300 mg at bedtime or 150 mg twice daily
(in the morning and at bedtime) is given initially for at least 4 weeks. A dose of 300 mg twice daily may also be used in duodenal ulcer.
Where appropriate a maintenance dose of 150 mg daily may be given at bedtime. Ranitidine 150 mg twice daily may be given during
therapy with NSAIDs for prophylaxis against duodenal ulceration.

A suggested dose for the treatment of peptic ulcer in children is 2 to 4 mg/kg twice daily to a maximum of 300 mg in 24 hours; a
maintenance dose of 2 to 4 mg/kg once daily may be used, to a maximum of 150 mg daily. For duodenal ulcer associated with Helicobacter
pylori infection, ranitidine in a usual oral dose of 300 mg once daily or 150 mg twice daily may be given as part of triple therapy with
amoxicillin 750 mg and metronidazole 500 mg, both three times daily, for 2 weeks. Therapy with ranitidine should then be continued for a
further 2 weeks.
In gastro-oesophageal reflux disease (p.1696) the oral dose is 150 mg twice daily or 300 mg at bedtime for up to 8 weeks or, if required,
12 weeks. This may be increased to 150 mg four times daily for up to 12 weeks in severe cases. In the maintenance of healing erosive
oesophagitis, a dose of 150 mg twice daily may be used. Although there is limited data on the use of ranitidine for gastro-oesophageal reflux
disease and erosive oesophagitis in children, a dose of 5 to 10 mg/kg daily, usually given in 2 divided doses, has been used. In pathological
hypersecretory conditions, such as the Zollinger-Ellison syndrome, (p.1704) the initial oral dose is usually 150 mg twice or three times
daily and may be increased if necessary; doses of up to 6 g daily have been used. Alternatively, an intravenous infusion may be given,
initially at a rate of 1 mg/kg per hour; the rate may be increased by increments of 500 micrograms/kg per hour, beginning after 4 hours, if
required.
For the management of patients at risk from stress ulceration of the upper gastrointestinal tract, parenteral therapy may be given as a slow
intravenous injection of a 50-mg priming dose followed by a continuous intravenous infusion of 125 to 250 micrograms/kg per hour. Oral
doses of 150 mg twice daily may be given once oral feeding is resumed.
In patients at risk of developing the acid aspiration syndrome (p.1693) during general anaesthesia, an oral dose of 150 mg may be given 2
hours before the induction of anaesthesia and preferably also 150 mg the previous evening. Alternatively, a dose of 50 mg may be given by
intramuscular or slow intravenous injection 45 to 60 minutes before the induction of anaesthesia. In obstetric patients, at the start of labour
an oral dose of 150 mg may be given and may be repeated at intervals of 6 hours if required. In patients with chronic episodic dyspepsia
(p.1695), a dose of 150 mg twice daily orally for up to 6 weeks may be given. For the short-term symptomatic relief of dyspepsia a dose of
75 mg, repeated if necessary up to a maximum of 4 doses daily, may be taken. Treatment should be restricted to a maximum of 2 weeks of
continuous use at one time.

Sucralfate is a cytoprotective drug that, under acid gastrointestinal conditions, forms an adherent complex with proteins which coats the
gastric mucosa and is reported to have a special affinity for ulcer sites. It also inhibits the action of pepsin and adsorbs bile salts. Sucralfate
has been used in the treatment of peptic ulcer disease (p.1702) and chronic gastritis. It is given orally and should be taken on an empty
stomach before meals and at bedtime. The usual dose is 1 g four times daily or 2 g twice daily for 4 to 8 weeks; if necessary the dose may be
increased to a maximum of 8 g daily.
If longer-term therapy is required sucralfate may be given for up to 12 weeks. Where appropriate a maintenance dose of 1 g twice daily may
be given to prevent the recurrence of duodenal ulcers. For prophylaxis of gastrointestinal haemorrhage from stress ulceration the usual dose
of sucralfate is 1 g six times daily; a dose of 8 g daily should not be exceeded. For children’s doses see below.
Uses and Administration
Ciprofloxacin is a fluorinated 4-quinolone or fluoroquinolone antibacterial with a wider spectrum of activity than nalidixic acid (see
Antimicrobial Action, above) and more favourable pharmacokinetics allowing its use in systemic infections. It has been used in the
treatment of infections including anthrax, biliary-tract infections, infected bites and stings, bone and joint infections, cat scratch disease,
chancroid, exacerbations of cystic fibrosis, ear, nose, and throat infections (including otitis externa, otitis media, and sinusitis), HACEK
endocarditis, gastro-enteritis (including travellers’ diarrhoea and campylobacter enteritis, cholera, salmonella enteritis, shigellosis, and
yersinia enteritis), gonorrhoea, granuloma inguinale, infections in immunocompromised patients (neutropenia), legionnaires’ disease, pelvic
inflammatory disease, peritonitis, plague, lower respiratory-tract infections (including pseudomonal infections in cystic fibrosis, but
excluding infections due to Streptococcus pneumoniae such as pneumococcal pneumonia), rickettsial infections (including Q fever, spotted
fevers, and typhus), septicaemia, skin infections (including soft-tissue infections), typhoid and paratyphoid fever, and urinary-tract
infections including chronic bacterial prostatitis. Ciprofloxacin is used for meningococcal meningitis prophylaxis. It is also used for surgical
infection prophylaxis and in the treatment of nontuberculous mycobacterial infections and tuberculosis. Ciprofloxacin is used topically in
the treatment of eye and ear infections.
For details of all these infections and their treatment, see under Choice of Antibacterial, p.162. Administration and dosage. Ciprofloxacin is
given orally as the hydrochloride or base, by intravenous infusion as the lactate, and in eye drops, eye ointment, or ear drops as the
hydrochloride. Doses and strengths are expressed in terms of the base. Ciprofloxacin hydrochloride 291.1 mg is equivalent to about 250 mg
of ciprofloxacin. Ciprofloxacin lactate 127 mg is equivalent to about 100 mg of ciprofloxacin.
The usual adult oral dose of ciprofloxacin ranges from 250 to 750 mg twice daily depending on the severity and nature of the infection.
Modified-release preparations for once-daily dosage are available in some countries. The usual adult intravenous dose is 200 to 400 mg
twice daily, given over 30 to 60 minutes as a solution containing the equivalent of 1 to 2 mg/mL. Women with acute uncomplicated cystitis
may be given an oral dose of 100 to 250 mg twice daily for 3 days or 100 mg twice daily by intravenous infusion. A 28- day course of
treatment with an oral dose of 500 mg twice daily or an intravenous dose of 400 mg twice daily should be given for chronic bacterial
prostatitis.
Bone and joint infections should be treated with an oral dose of 500 to 750 mg twice daily or an intravenous dose of 400 mg two or three
times daily for 4 to 6 weeks. Intravenous infusions of 400 mg three times daily have also been recommended in severe or complicated lower
respiratory tract or skin infections, nosocomial pneumonia, and with piperacillin for empirical treatment of febrile neutropenic patients.

For treatment and postexposure prophylaxis of inhalation anthrax, a 60-day course of treatment with initial intravenous doses of 400 mg
twice daily followed by oral doses of 500 mg twice daily is recommended; although unlicensed, the same regimen is recommended by UK
and US public health agencies for the treatment of gastrointestinal anthrax. In the treatment of cutaneous anthrax (also unlicensed), a 7- to
10-day course of treatment with an oral dose of 500 to 750 mg twice daily is similarly recommended; treatment may need to be extended to
60 days if infection is due to aerosol exposure.
Doses should be reduced in patients with severe renal
impairment (see below).
Single oral doses of 250 or 500 mg or single intravenous doses of 100 mg are used for the treatment of
gonorrhoea, depending upon patterns of resistance. A
single oral dose of 750 mg is used for surgical infection
prophylaxis, given 60 to 90 minutes before the procedure. Although unlicensed in the UK, the BNF suggests a single oral dose of 500 mg for
meningococcal
meningitis prophylaxis.
For details of doses in children, including infants and
adolescents, see below.
For corneal ulcers and superficial ocular infections
caused by susceptible strains of bacteria ciprofloxacin
is given as the hydrochloride in eye drops and eye ointment containing the equivalent of 0.3% of ciprofloxacin.
Ciprofloxacin is also used topically as the hydrochloride in ear drops containing the equivalent of 0.2 or
0.3% of ciprofloxacin, usually with a corticosteroid
such as dexamethasone or hydrocortisone, for the treatment of otitis externa and chronic suppurative otitis
media caused by susceptible strains of bacteria.

Cefixime is generally classified as a third-generation

cephalosporin antibacterial and is given orally in the
treatment of susceptible infections including gonorrhoea, otitis media, pharyngitis, lower respiratory-tract
infections such as bronchitis, and urinary-tract infections. For details of these infections and their treatment, see under Choice of
Antibacterial, p.162.
Cefixime is available as the trihydrate and doses are
expressed in terms of anhydrous cefixime; 1.12 g of
cefixime trihydrate is equivalent to about 1 g of anhydrous cefixime. It is given orally in adult doses of 200
to 400 mg daily as a single dose or in two divided doses. Children over 6 months and under 50 kg may be
given 8 mg/kg daily as an oral suspension, again as a
single dose or in two divided doses. For details of reduced dosage of cefixime in patients with moderate to
severe renal impairment, see below.
For uncomplicated gonorrhoea, a single oral dose of
400 mg is given.

Levofloxacin is the S-(-)-isomer of the fluoroquinolone antibacterial ofloxacin (p.310). It is given orally, or
by intravenous infusion as a 5 mg/mL solution over 30
to 90 minutes, to treat susceptible infections including
tuberculosis (but see under Uses and Administration of
Ciprofloxacin, p.248). Levofloxacin is given as the
hemihydrate but doses are expressed in terms of the
base; levofloxacin hemihydrate 256 mg is equivalent
to about 250 mg of levofloxacin. Usual doses range
from 250 to 500 mg once or twice daily for 7 to 14 days
depending on the severity and nature of the infection.
A dose of 250 mg once daily for 3 days may be given
for uncomplicated urinary-tract infections. A 28-day
course of treatment with a dose of 500 mg once daily
should be given for chronic bacterial prostatitis. In the
USA, doses of 750 mg once daily for 7 to 14 days may
be used for complicated skin infections and for hospital-acquired pneumonia; a shorter course of 750 mg
once daily for 5 days may be given for community-acquired pneumonia, acute bacterial sinusitis, complicated urinary-tract infections, and
acute pyelonephritis. A
60-day course of treatment with a dose of 500 mg once
daily is also licensed in the USA for treatment and postexposure prophylaxis of inhalation anthrax.
Doses should be reduced in patients with renal impairment (see below).
Levofloxacin is also used topically as the hemihydrate
in eye drops. A solution containing the equivalent of
0.5% of levofloxacin is used for the treatment of bacterial conjunctivitis and 1.5% for corneal ulcers caused
by susceptible strains of bacteria.
Cefadroxil is a first-generation cephalosporin antibacterial that is the para-hydroxy derivative of cefalexin
(p.219), and is used similarly in the treatment of mild
to moderate susceptible infections. It is given orally,
and doses are expressed in terms of the anhydrous substance; 1.04 g of cefadroxil monohydrate is equivalent
to about 1 g of anhydrous cefadroxil. The usual adult
dose is 1 to 2 g daily as a single dose or in two divided
doses. The following doses are used in children weighing less than 40 kg: 500 mg twice daily for those over
6 years of age, 250 mg twice daily for those aged 1 to
6 years, and 25 mg/kg daily in divided doses for infants
under 1 year. For details of reduced doses of cefadroxil
in patients with renal impairment, see below.
Cefadroxil has also been used as the lysine derivative.

Rebamipide is stated to possess cytoprotective properties and is

used in the treatment of peptic ulcer disease (p.1702) and gastritis
in usual oral doses of 100 mg three times daily. It has also been
used rectally for the treatment of intestinal inflammation. Rebamipide eye drops are under investigation in the treatment of
dry eye.
Ondansetron is a 5-HT3 antagonist (5-HT3-receptor
antagonist) with antiemetic activity. It is used in the
management of nausea and vomiting induced by cytotoxic chemotherapy and radiotherapy. It is also used
for the prevention and treatment of postoperative nausea and vomiting. For the management of nausea and
vomiting, and the important role of 5-HT3 antagonists,
see p.1700.
Ondansetron is given by intramuscular or slow intravenous injection or infusion as the hydrochloride, by
mouth as the hydrochloride or base, or rectally as the
base. Doses are expressed in terms of the base. On dansetron hydrochloride 4.99 mg is equivalent to
about 4 mg of ondansetron base.
Numerous dosing schedules of ondansetron have been used; some typical examples are cited below. For highly emetogenic chemotherapy
the following dose schedules appear to be equally effective in preventing acute emesis:
• a single dose of 8 mg by slow intravenous or intramuscular injection immediately before treatment
or
• 8 mg by slow intravenous or intramuscular injection immediately before treatment, either followed by a continuous intravenous infusion of
1 mg/hour for up to 24 hours, or by a further two doses of 8 mg two to four hours apart
or
• a single dose of 32 mg given by intravenous infusion over at least 15 minutes immediately before treatment
or
• 150 micrograms/kg by intravenous infusion over 15 minutes, beginning 30 minutes before chemotherapy, and repeated 4 and 8 hours after
the first dose
or
• a 16-mg suppository rectally, given 1 to 2 hours before treatment
or
• a single oral dose of 24 mg taken 30 minutes before the start of single-day chemotherapy. The efficacy of ondansetron in highly
emetogenic chemotherapy may be enhanced by giving intravenous dexamethasone sodium phosphate 20 mg before chemotherapy.
Similar regimens to those given above are used for preventing acute emesis with less emetogenic chemotherapy and/or radiotherapy and
also include:
• 8 mg can be given orally up to 2 hours before treatment followed by 8 mg 8 to 12 hours later

To protect against delayed emesis these regimens are followed by oral ondansetron 8 mg twice daily, or 16 mg rectally once daily, for up to
5 days after the end of a course of chemotherapy.
For children the licensed dose in the UK is 5 mg/m2 intravenously immediately before chemotherapy, followed by 4 mg orally 12 hours
later. A dose of 4 mg orally twice daily may be continued for up to 5 days after the end of chemotherapy. The BNFC allows (in children
aged 1 to 12 years) for 5 mg/m2 intravenously before chemotherapy (up to a maximum single dose of 8 mg), which can be repeated every 8
to 12 hours during chemotherapy and for at least 24 hours afterwards; alternatively oral doses of 4 mg can be given every 8 to 12 hours for
up to 5 days after intravenous use. In the USA a licensed regimen in children over 6 months of age is 150 micrograms/kg by intravenous
infusion 30 minutes before chemotherapy, repeated 4 and 8 hours after the first dose. Alternatively, for children aged 4 to 11 years, an oral
dose of 4 mg may be given 30 minutes before the start of chemotherapy, with subsequent 4-mg doses given 4 and 8 hours thereafter. An oral
dose of 4 mg three times daily may be given for 1 to 2 days after the end of chemotherapy.
To prevent postoperative nausea and vomiting adults may be given:
• 16 mg orally an hour before anaesthesia
or
• 8 mg orally an hour before anaesthesia followed by 2 further doses of 8 mg at 8-hour intervals
or
• a single dose of 4 mg by intramuscular or slow intravenous injection at induction of anaesthesia
For the treatment of postoperative nausea and vomiting a single 4-mg dose by intramuscular or slow intravenous injection is recommended.
In the UK, children aged 2 years and over may be given 100 micrograms/kg by slow intravenous injection, up to a maximum dose of 4 mg,
both for the prevention and treatment of postoperative nausea and vomiting; in the USA this dose is licensed from 1 month of age. In
patients with moderate or severe hepatic impairment it is recommended that the total daily dose of ondansetron should not exceed 8 mg (see
below).

Domperidone is a dopamine antagonist with actions and uses similar to those of metoclopramide (p.1749).
It is used as an antiemetic for the short-term treatment of nausea and vomiting of various aetiologies (p.1700).
It is not considered suitable for chronic nausea and vomiting, nor for the routine prophylaxis of postoperative vomiting.
Domperidone is also used for its prokinetic actions in dyspepsia (p.1695) and has been tried in diabetic gastroparesis (see Diabetic
Complications, p.433). It has been given with paracetamol in the symptomatic treatment of migraine (p.616).
Domperidone is used as the maleate in tablet preparations and as the base in suppositories and the oral suspension; doses are expressed in
terms of the base.
Domperidone maleate 12.73 mg is equivalent to about 10 mg of domperidone. Domperidone has been given parenterally, but this route has
been associated with severe adverse effects (see above).
For the treatment of nausea and vomiting domperidone may be given in oral doses of 10 to 20 mg three or four times daily up to a
maximum daily dose of 80 mg or it may be given rectally in a dose of 60 mg twice daily. For doses in children see below.
For the symptomatic management of non-ulcer dyspepsia similar oral doses of 10 mg taken up to four times daily (the last dose to be taken
at night) have been recommended; if necessary, an increase in the dose to 20 mg may be prescribed. An initial course of treatment should
not normally exceed 2 to 4 weeks. In migraine, a dose of 20 mg has been given orally up to every 4 hours, with paracetamol, as required, up
to a maximum of 4 doses in 24 hours.
Metoclopramide hydrochloride is a substituted benzamide used for its prokinetic and antiemetic properties.
It stimulates the motility of the upper gastrointestinal
tract without affecting gastric, biliary, or pancreatic secretion and increases gastric peristalsis, leading to accelerated gastric emptying.
Duodenal peristalsis is also
increased which decreases intestinal transit time. The
resting tone of the gastro-oesophageal sphincter is increased and the pyloric sphincter is relaxed. Metoclopramide possesses
parasympathomimetic activity as
well as being a dopamine-receptor antagonist with a direct effect on the chemoreceptor trigger zone. It may
have serotonin-receptor (5-HT3) antagonist properties.
Metoclopramide is used in disorders of decreased gastrointestinal motility (p.1694) such as gastroparesis or
ileus; in gastro-oesophageal reflux disease (p.1696)
and dyspepsia (p.1695); and in nausea and vomiting
(p.1700) associated with various gastrointestinal disorders, with migraine, after surgery, and with cancer therapy. Metoclopramide is of no
value in the prevention or
treatment of motion sickness. It may be used to stimulate gastric emptying during radiographic examinations, to facilitate intubation of the
small bowel, and in
the management of aspiration syndromes (p.1693).
It is usually given as the hydrochloride monohydrate
with doses expressed as the anhydrous hydrochloride.
In the USA, the strength of preparations of the hydrochloride monohydrate is usually expressed in terms of
the base. Metoclopramide hydrochloride 10.5 mg is
equivalent to about 10.0 mg of the anhydrous substance, which is equivalent to about 8.9 mg of the
anhydrous base.
For most purposes the total daily dose should not exceed 500 micrograms/kg; dosage reduction is recommended in renal and perhaps hepatic
impairment (see
Administration in Hepatic or Renal Impairment, below).
• In the UK, the recommended dose orally, intramuscularly, or by slow intravenous injection, is 10 mg
(expressed as anhydrous metoclopramide hydrochloride) three times daily.
• In the USA, the recommended dose is 10 to 15 mg
(expressed as the base) up to four times daily.
• Single doses of 10 to 20 mg (expressed as anhydrous
base or anhydrous hydrochloride) should be considered where appropriate.
Modified-release preparations of metoclopramide are
available; 15 mg (expressed as anhydrous metoclopramide hydrochloride) is given twice daily.
In the UK, the use of metoclopramide is restricted in
patients under 20 years of age (see Administration in
Children, below).
An intranasal formulation of metoclopramide is available in some countries.
The base, the dihydrochloride, and the glycyrrhizate
have also been used.
High-dose therapy. High doses of metoclopramide
have been used, often with other drugs such as dexamethasone, in the treatment of the nausea and vomiting
associated with cancer chemotherapy. The loading
dose of metoclopramide before cancer therapy is 2 to
4 mg/kg given as a continuous intravenous infusion
over 15 to 20 minutes; it is followed by a maintenance dose of 3 to 5 mg/kg, again as a continuous intravenous
infusion, given over 8 to 12 hours. Alternatively, initial
doses of up to 2 mg/kg by intravenous infusion over at
least 15 minutes may be given before cancer therapy
and repeated every 2 or 3 hours. The total dosage by
either continuous or intermittent infusion should not
normally exceed 10 mg/kg in 24 hours.