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Allopathic
Medicines
The
importance of allopathic medicines cannot be denied
in all forms of diseases, whether acute or chronic.
However, all drugs have side-effects and should not be taken
without the advice of a physician. Allopathic
medicines that are in use in case of Arthritis and related conditions are
:
Anti-inflammatory drugs
-
Non-steroid
anti-inflammatory drugs (NSAIDs)
-
Corticosteroids
Disease-modifying ant-rheumatic drugs (
DMARDs)
Topical analgesics
Drugs for gout
-
Acute
gout: NSAIDs, Cortiocosteroids, Colchines
-
Chronic
gout or hyperuricemia
Uricosourics : Probenecid, Sulfinpyrazone
Synthesis inhibitor: Allopurinol
Glucosomine and Chondroitin sulpate
1.
Anti-inflammatory Drugs
1a)
Non-steroid Anti-inflammatory Drugs ( NSAIDs)
These
groups of drugs are used as the first line of treatment in most cases of
Arthritis and related conditions. This
medication helps by both decreasing pain and inflammation in an arthritic
joint. They are divided into
various groups as per their individual and similar properties. They
share certain therapeutic actions and side-effects.
Taking more than one NSAID at a time increases the possibility of
side-effects, particularly stomach problems, such as heartburn, ulcers and
bleeding. All NSAIDs
should be used with caution in patients of impaired renal or
cardiac function or patients with previous history of peptic ulcer and in
elderly.
Adverse
Effects of NSAIDs
q
Gastrointestinal
ulceration ( less with paraaminophenol derivatives)
q
Barricade of
platelet aggregate.
q
Elevation of blood
pressure
q
Allergic reaction (
more with aspirin)
Interaction
of NSAIDs with other Drugs
q
Methotrexate: Risk of methotrexate toxicity may be increased.
q
Cyclosporine : Nephrotoxicity of both agents may be increased.
q
Lithium : Serum lithius levels may be increased leading to
toxicity.
q
Anticoagulants: Risk of increased bleeding.
q
ACE inhibitors: Antihypertensive effects of captropril may be
abolished by indomethacin.
q
B-Blockers: Antihypertensive effects maybe blunted.
q
Digoxin : Serum digoxin levels may be increased by ibuprofen and
indomethacin.
q
Hydantoins : Serum hydantoin levels increased resulting in
increased pharmacological and
toxic effects.
Types
of NSAIDs
I.
Salicylates : Aspirin
II.
Propionic acid derivatives : Ibuprofen, Flubriprofen, Ketoprofen,
Naproxen.
III.
Fenamates ( Anthranilic Acides): Mefanamic acid
IV.
Pyrazolones : Phenylbutazone, Oxyphenbutazone
V.
Indol derivatives : Indomethacin
VI.
Aryl acetic acid derivatives : Diclofenac
VII.
Oxicam derivatives : Piroxicam, Tenoxicam
VIII.
Pyrrolo-pyrrole derivatives : Ketorolac
IX.
Paraaminophenol derivatives : Phenacetin, Paracetamol
X.
Others : Celecosib, Rofecoxib, Nimesulide, Serratiopeptidase.
1
a-I) Aspirin
It
is one of the most usable drugs in pain, especially headache.
It should be avoided with other NSAIDs.
Allergic reaction to aspirin, though less, at times may be serious,
leading to urticaria, angioedema, and rashes.
It should not be given to children as it may lead to Reye’s
syndrome. It is
contraindicated in patients with
peptic ulcer, bleeding tendency, chronic liver disease, diabetes and
juvenile rheumatoid Arthritis. Breastfeeding
mothers and pregnant women should also avoid it.
It
has interaction with other drugs. It
increases hypoglycaemic effects of oral hypoglycaemic.
It should not be given with oral anticoagulants as it may increase
the risk of bleeding of patients. Concomitant
use with phenytoin, warfarin, methotrexate, and naproxen may result in
toxicity.
The
usual dosage is 300 mg to 600 mg thrice daily in case of headache,
backache, joint pain, fever and dysmenorrhoea.
It is the first line drug in case of rheumatic level.
It is also given in post-stroke patients and in pregnancy
associated with hypertension. Higher
doses up to 3 gm per day may be given to some patients but if there are
nay side-effects including vertigo or tinnitus, the dose should be reduced
and adjusted as per the patient.
1a-ii)
Ibuprofen
It
is used in the treatment of rheumatoid Arthritis, osteoarthritis,
ankylosing spondylitis, and cervical spondylosis.
Combined preparations with paracetamol are also used for the same
purpose. It is
contraindicated in case of peptic ulcer.
The
usual dosage is 400 mg thrice daily for adults.
The maximum dose is 2.4 g daily.
For children, it is 10-15 mg/kg/day every 4-6 hours.
In case of juvenile rheumatoid Arthritis, it is 20-40 mg/kg/day in
3-4 divided doses.
1a–iii)
Mefenami Acid
It
has got analgesic, anti-inflammatory and antipyretic properties.
It is indicated in joint and soft tissue pain, rheumatoid Arthritis
and Osteoarthritis. It is
contraindicated in peptic ulcer and inflammatory bowel disease.
The
usual dosage is 250-500 mg thrice daily, preferable
after food for adults. For
children, it is 10-25 mg/kg/day in divided doses.
The therapy should not exceed more than seven days.
1a-iv)
Phenylbutazone
It
is a potent anti-inflammatory drug. It
is used in the treatment of rheumatoid Arthritis, osteoarthritis,
ankylosing spondylitis, acute gout. It
is contraindicated in peptic ulcer, hypertension, congestive heart
failure, impairment of liver and kidney function, hypersensitivity, blood
dyscrasias, theyroid disease. It
should be used only after other drugs have failed. It may produce sodium
and wter retention andmust be used with caution inpatients with cardiac
insufficiency. It may also
lead to bone marrow damage. Always check blood count
periodically, if this drug is in use.
It
has high interaction with other drugs.
Duration of effect and toxicity of drugs such as anti-inflammatory
agents, oral anticoagulants, oral anti-diabetics, sulfonamides, sodium
valproate and phenytoin may
be increased
Initially,
it is given in the dose of 200 mg 2-3 times daily for 2 days, with or
after food, then reduced to minimum effective dose, usually 100 mg 2-3
times daily. It is not recommended for children under fourteen years of
age.
1a-v)
Indomethacin
It
is a potent anti-inflammatory drug with antipyretic and analgesic action.
It is used in the treatment of
rheumatoid Arthritis, osteoarthritis, ankylosing spondylitis, and gout.
It is contraindicated in peptic ulcer, epilepsy, Parkinsonism,
renal disease, psychiatric patients and hypersensitivity.
Fluid retention is possible in elderly.
The
usual dosage is 25 mg thrice daily. It is not recommended for children.
1a-vi)
Diclofenac
It
is a very commonly used non-steroidal anti-inflammatory drug.
It has analgesic, antipyretic and anti-inflammatory actions. It is used in the treatment of rheumatoid Arthritis,
osteoarthritis, low back pain, ankylosing spondylitis, gout, acute
musculoskeletal disorders, periarthritis ( froxen shoulder) tendonitis,
tenosynovitis, bursitis, painful post-operative conditions.
It
is contraindicated in peptic ulcer, NSAID- induced allergic asthma.
Enhanced toxicity with drugs like digoxin, lithium, methotrexate,
hydantoins, and cyclosporine.
The
usual dosage is 100-150 mg daily in 2-3 divided doses for adults.
It is not recommended for children.
1a-vii)
Piroxicam
It
is an effective anti-inflammatory drug.
It is used in the treatment of rheumatoid Arthritis, osteoarthritis,
ankylosing spondylitis, acute musculo-skeletal disorders and acute gout.
It is contraindicated in peptic ulcer, NSAID-induced allergy,
hypersensitivity, and bronchial asthma.
It
has high interaction with other drugs.
Duration of effect and toxicity of thedrugs such as methotrexate,
cyclosporin, hydantoins, and lithium may be increased .
Probenecid may increase
the concentration and toxicity of piroxicam.
Aspirin displaces piroxicam from serum binding site resulting in
increased incidence of gastrointestinal effects.
The
usual dosage is 20 mg daily as a single dose
for adults. In case of
gout, 40 mg can be given initially for first two days and then 20 mg once
daily. Injection is given same as oral dose by deep intramuscular
injection into upper, outer quadrant of buttocks.
It is not recommended for children.
1a-viii)
Paracetamol ( Acetaminophen)
It
has analgesia and anti-pyretic effects.
It has negligible anti-inflammatory action in therapeutic doses.
IT is indicated in all types of pain and fever.
It is contraindicated in analgesic nephropathy.
It should not be used for long-term as it may lead to chronic renal
disease. People with liver
disease, those who drink alcohol heavily, and those taking blood-thinning
medicines or NSAIDs should use acetaminophen with caution.
The
usual dosage is 500 mg-1gm 3-6 times daily for adults.
The dose should not exceed more than 4 gm.
For children, the dose is 15 mg/kg/dose or 60 mg/kg/day divided
every 6 hours. In a day, the maximum number of doses should be five.
However, it is generally given on
S.O.S. basis, i.e., if necessary.
1a-ix)
Celecoxib
It
is non-steroidal anti-inflammatory drug having less gastrointestinal
side-effects. It is used in
the treatment of rheumatoid. Arthritis
and osteoarthritis. It is
contraindicated if the patient has allergic reaction to it or any other
NSAIDs.
The
usual dosage is 200 mg per day in single or 2 divided doses for adults.
It is not recommended for children.
1a-x
) Nimesulide
It
is one of common Non-steroidal anti-inflammatory drugs with high degree of
analgesia and antipyretic effects. The
advantage of nimesulide over than NSAIDs is that is causes minimal gastric
irritation. It is indicated
in all types of pain, rheumatoid Arthritis, osteoarthritis, and lumbago.
It is contraindicated in case of peptic ulcer and moderate to
severe liver disease.
The
usual dose is 100 mg twice daily for adults.
For children, it is 5 mg/kg/day divided into two doses.
1b)
Corticosteroids
Corticosteroids
are man-made drugs that closely resemble cortisone.
Cortisone is a steroid that reduces inflammation and swelling. It is a hormone naturally produced by the body.
Corticosteroid has been used in rheumatoid Arthritis,
osteoarthritis, ankylosing spondylitis and in all types of
pain that are intolerable. However,
because of potential long-term side-effects including osteoporosis and
coronary artery disease, corticosteroid use is limited
to short courses and low doses where possible.
They are indicated when patients do not respond to NSAIDs.
They have potent immunosuppressant and anit-inflammatory activity.
They can be used at any stage in rheumatoid Arthritis if potent
anti-inflammatory action is required.
However, they do not arrest the rheumatoid process to prevent
erosions.
The
adverse effect of corticosteroid in brief
may include high blood pressure, osteoporosis, diabetes, cataracts
and susceptibility to infections. Corticosteroids
can be taken either by mouth or given by injection.
Corticosteroids may be injected into the affected joints to provide
immediate relief for a tender, swollen and inflamed joint.
This is a short-term measure, generally not recommended for more
than two or three treatments per year.
Oral corticosteroids should not be used to treat osteoarthritis.
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2.
Disease Modifying Anti-rheumatic Drugs ( DMARDs)
DMARDs
are another type of drug used to treat people with rheumatoid Arthritis who
have not responded to NSAIDs. They
take about two to six months before they begin to make a difference
in the pain and swelling. They
are prescribed when inflammation continues for more than two months. A DMARD is usually prescribed in addition to an NSAID or
corticosteroid. They require
careful monitoring by the physician due to their side-effects.
The decision to treat patients with DMARDs should be taken only by a
physician having experience of their use.
Most
Common Types of DMARDs
-
Gold
-
D-Pencillamine
-
Sulfasalazine
-
Hydroxychloroquine,
chloroquine
2a)
Gold
It
prevents damage to cartilage and is used in the treatment of rheumatoid
Arthritis, psoriatic arthopathy and juvenile Arthritis.
Side-effects include pruritis, dermatitis,
peripheral neuritis, renal and liver damage, thrombocytopenia and neutropenia.
Vasodilation and postural hypotension occur after a dose.
Due to its side-effects, it is essential to monitor blood counts and
urinary protein. Women in
reproductive age group should use effective contraception during the therapy
and upto six months after the therapy is stopped.
It is contraindicated in liver disease, chronic renal disease and
pregnancy. There is an increased
risk of toxicity with pehnytoin and other nephrotoxic drugs.
With oral preparation, the side-effects are less and mainly include
diarrhoea, pruritis and abdominal cramps.
The
usual dosage for oral preparations is 6 mg daily in two divided doses (
morning and evening) or as a single ( in morning ) dose for minimum 3-6
months. It is not recommended for
children. In injectable form, it
is given as intramuscular ( i.m.). The
starting dose of 10 mg i.m. per week is gradually increased to 50 mg i.m. per
week. The maximum total dose is 1
g.
2b)
D-Pencillamine
It
is a copper-chelating agent used in the treatment of rheumatoid Arthritis.
Its toxicity is similar to that of gold but it is less effective. Side-effects include allergic reaction, proteinuria,
thrombocytopenia, drug-induced SLE, myasthenia gravis, pemphigus reaction, and
Good pasture’s syndrome. Periodical
check of blood count and urinalysis is required for monitoring.
It should not be given concurrently with gold salts, antimalarial drugs
and phenylbutazone.
The
starting dose is 250 mg once daily, which may be increased to 250 mg twice
daily. It is not recommended for
children. It is also indicated in
Wilson’s disease and scleroderma.
2c)
Sulfasalazine
It
is indicated in rheumatoid Arthritis and has lesser side-effects than gold or
d-pencillamine. Its effectiveness is similar to that of hydrochloroquine.
Side-effects include haemolytic anaemia, allergic reaction, hepatitis,
pulmonary eosinophilia, and reduced sperm count.
The usual dosage is 1 to 2 gm per day in two doses.
2d)
Hydroxychloroquine
It
is an antimalarial drug that is used in milder cases of rheumatoid Arthritis,
not responding to NSAIDs. It is
to be given for a long time so that it can become effective in rheumatoid
Arthritis. The most important
side-effect of this drug is retinal damage and
corneal opacity.
Hence, patients taking this drug are required to have ophthalmology
check-up every 6 months. Other
adverse effects are rashes, graying of hair, irritable bowel syndrome,
myopathy and neuropathy. The
starting dose is 400 mg per day, which can be brought down to 200 mg per day
as maintenance dose.
There
are other drugs that are effective in rheumatoid Arthritis such as
azathioprine, methotrexate, cyclophosphamide and cyclosporine.
But due to their high toxicity, these drugs are reserved for patients
not responding to the drugs mentioned above.
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3.
Tropical Analgesics
The
principal drugs used in topical analgesics are salicylates, capsicum,
nicotinates and histamine. Camphor and menthol are also added in some preparations
that produce a feeling of coolness.
These topical agents also contain drugs like Ibuprofen, Mephenesin,
Diclofenac, Piroxicam, Nimesulide and Phenylbutazone.
These preparations are for external use only.
They produce soothing sensation, tingling and warmth.
Topical
analgesics are indicated for the temporary relief of minor aches and pain of
muscles and joints due to muscle strains, sprains and bruises or overexertion,
as an adjunct in the management of minor stiffness or soreness associated with
Arthritis, rheumatism, lumbago, fibrositis, sciatica and stiff neck.
Topical
analgesic, just like any other medicine, also has adverse effects. It may
cause dermatitis, local irritation erythema, photosensitivity, and pruritus.
Topical analgesics containing salicylates are to be avoided or used
with caution in patients of Vitamin K deficiency, hypothrombinemia, and liver
disease and before surgery. It is
not to be applied on wounds and broken skin.
It is to be used under medical supervision during pregnancy and
lactation. As the drugs in
topical analgesics may produce irritation, they should not be applied near the
eyes, on the mucus membrane or on inflamed skin.
The
usual dosage is to apply it to the affected area 2-3 times daily.
Rubbing or massaging should be usually avoided.
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4.
Drugs for Gout
4a)
Colchincine
Colchicine
is a medication that has been used since the 1800s to treat gout.
It is an alkaloid from colchicum autumnale.
It is very effective in suppressing gouty inflammation. But it does not promote the excretion of uric acid.
Adverse effects include nausea, vomiting, abdominal cramps and
diarrhoea. Potential bone marrow
toxicity limits the use of intravenous colchicines for acute gout.
However, it may be prescribed for patients who have contraindications
for both NSAIDs and corticosteroids. In
overdose, colchicines produces kidney damage, CNS depression and intestinal
bleeding and may also result in
death due to muscular paralysis and respiratory failure.
Colchicine is not used for long-term therapy as it causes aplastic
anaemia and agranulocytosis.
4b)
Probenecid
In
case of chronic gout, probenecid is given to bring the uric acid to normal
levels. It should not be taken
with salicylates. Side-effects are well tolerated among which dyspepsia is
common. It is contraindicated in
renal disease, and uric acid stones. It
is given at a dose of 250 mg twice daily and increased to 500 mg twice daily
after a week. The maximum dose is
1 gm twice daily. If you are
taking probenecid, you must drink sufficient water to
reduce the risk of kidney stones; drink at least 4 to 5 glasses of
water daily. It should not be
given in case of acute gout.
4c)
Sulfinpyrazone
It
is used in chronic gout having marked uricosuric action.
It inhibits platelet aggregation and has been used for secondary
prophylaxis of arterial thrombosis. The
most common side-effect of the drug is gastric irritation. It is
contraindicated in patients with peptic ulcer.
It is given in the dose of 200 mg twice daily that is increased
gradually to the maximum dose of 400 mg twice daily.
4d)
Allopurinol
Allopurinol
is given in chronic gout to lower serum uric acid levels.
But it will not relieve an attack that has already started.
Thus, the time for allopurinol is after a gouty flare has calmed down;
it should not be started for two to three weeks after symptoms have resolved.
If started too soon, allopurinol could exacerbate a gouty flare.
Because its action causes a reduction in both blood and urine levels of
uric acid, allopurinol is used in the treatment of gout when the patient has
had kidney stones related to uric acid, or when tophi are present.
Concomitant
use of iron therapy with allopurinol is not recommended.
It is also not given with ampicillin as it may result in skin rashes. It is contraindicated in hypersensitive patients, bone marrow
depression, and pregnancy. It is
also used in secondary hyperuricemia due to cancer chemotherapy.
Allopurinol is given at a dose of 100 mg three times daily and
increased by 100 mg weekly up to the maximum dose of 600 mg per day.
It should not be given during acute attacks of gout.
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5.
Glucosamine and Chondroitin
Sulphate
Glucosamine
and chondroitin sulphate are found in the synovial fluid of the knee.
Several studies have reported some pain relief and improved function
from taking either one or a combination of the two natural substances. They are indicated in the treatment of osteoarthritis of
knees.
Glucosamine
sulphate is an artificially synthesized salt of glucosamine that has been
known in animal studies to have the potential to slow the rate of cartilage
degradation. Glucosamine is an
amino sugar, produced by the body and involved in the maintenance and repair
of articular cartilage. It is
believed that glucosamine stimulates cartilage cells to produce
glycosaminoglycans and proteoglycans, which are the building blocks of
cartilage. By this mechanism, it
is thought to stop the progression of osteoarthritis and possibly reverse the
process. It has also been
reported that glucosamine has anti-inflammatory properties produced by its
inhibition of proteolytic enzymes.
The
recommended dose of oral glucosamine and chondrointin sulfate is 1,500 mg of
glucosamine and 1,200 mg of chondroitin sulfate divided equally in 3
doses. It should be given
for 3 months.
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