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Sulfasalazine, Uses, Dosage, Side Effects, Interactions, Pregnancy

Sulfasalazine is a synthetic salicylic acid derivative with affinity for connective tissues containing elastin and formulated as a prodrug, antiinflammatory Sulfasalazine acts locally in the intestine through its active metabolites, sulfamide 5-aminosalicylic acid and salicylic acid, by a mechanism that is not clear. It appears inhibit cyclooxygenase and prostaglandin production and is used in the management of inflammatory bowel diseases.

Sulfasalazine a drug that is used in the management of rheumatoid arthritis, ulcerative colitis, and Crohn’s disease, inflammatory bowel diseases. It is often considered as a first line treatment in rheumatoid arthritis. It is taken by mouth. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid released in the colon

Mechanism of Action of Sulfasalazine

The mode of action of Sulfasalazine or its metabolites, 5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), is still under investigation, but may be related to the anti-inflammatory and/or immunomodulatory properties that have been observed in animal and in vitro models, to its affinity for connective tissue, and/or to the relatively high concentration it reaches in serous fluids, the liver, and intestinal walls, as demonstrated in autoradiographic studies in animals. In ulcerative colitis, clinical studies utilizing rectal administration of Sulfasalazine, SP, and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety. The relative contribution of the parent drug and the major metabolites in rheumatoid arthritis is unknown.

The purpose of the present study was to determine whether sulfasalazine therapy affected NF-kappaB activation and the expression of pro-inflammatory cytokines in patients with ulcerative colitis. … A total of 38 patients with moderate ulcerative colitis were investigated. Twenty-one patients received sulfasalazine. Seventeen patients did not receive any medication. Biopsy specimens were obtained from the inflamed mucosa and analyzed for NF-kappaB DNA binding activity, NF-kappaBp65/IkappaBalpha protein expression and the levels of pro-inflammatory cytokine mRNA using electrophoretic mobility shift assay, western blot analysis, immunohistochemical staining and reverse transcription-polymerase chain reaction (RT-PCR) analysis, respectively. Increased activation of NF-kappaB and high levels of the expression of interleukin (IL)-1beta mRNA and IL-8 mRNA were detected in biopsy specimens from patients with ulcerative colitis. Therapeutic administration of sulfasalazine effectively downregulated the activation of NF-kappaB and the expression of IL-1beta mRNA and IL-8 mRNA while IkappaBalpha levels were stable. /The authors concluded that/ the therapeutic benefits for ulcerative colitis of sulfasalazine might at least in part be attributed to its ability to inhibit NF-kappaB activation, resulting in the downregulation of pro-inflammatory cytokine mRNA expression.

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Indications of Sulfasalazine

For the treatment of Crohn’s disease and rheumatoid arthritis as a second-line agent.
Rheumatoid Arthritis
Ankylosing Spondylitis
Multiple joint pain
Morning stiffness
Inflammatory Bowel Disease
Crohn’s Disease
Juvenile Rheumatoid Arthritis
Lymphocytic Colitis
Psoriatic Arthritis
Ulcerative Colitis
Polyarticular juvenile rheumatoid arthritis, chronic or unspecified
Proctitis
Mild Ulcerative Colitis
Alopecia

Contra-Indications of Sulfasalazine

Patients with intestinal or urinary obstruction, Patients with porphyria as sulfonamides have been reported to precipitate an acute attack, Patients hypersensitive to sulfasalazine, its metabolites, sulfonamides, or salicylates.

Severe infection
Glucose-6-Phosphate Dehydrogenase Deficiency
Porphyria
Low Blood Counts due to Bone Marrow Failure
Decreased Neutrophils a Type of White Blood Cell
Asthma
Stomach or Intestine Blockage
Liver Problems
Kidney disease with reduction in kidney function
Urinary Tract Blockage
Anemia from Pyruvate Kinase and Deficiencies
Slow Acetylator

Allergies

Salicylates
NSAIDs (Non-Steroidal Anti-Inflammatory Drug)
Sulfa (Sulfonamide Antibiotics)
Sulfasalazine

Dosage of Sulfasalazine

Strength: 500 mg, 1000 mg

Rheumatoid Arthritis

Delayed-release tablets: 1000 mg orally twice a day

Suggested dosing regimen

Week 1: 500 mg orally once a day in the evening
Week 2: 500 mg orally twice a day (morning and evening)
Week 3: 500 mg orally in the morning and 1000 mg in the evening
Week 4: 1000 mg orally twice a day (morning and evening)
For maintenance therapy, the dose is 2,000 mg per day taken in 2 evenly divided and evenly spaced doses.

Ulcerative Colitis

3 to 4 g/day orally in evenly divided doses

Crohn’s Disease

3 to 6 g/day orally in divided doses

juvenile rheumatoid arthritis

The maintenance dose is 30–50 mg/kg of body weight per day taken in two evenly divided and evenly spaced doses.

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Uveitis

Initial dose: 500 mg/day, then increased by 500 mg/week
Maintenance dose: 1 g twice a day for 1 year; in cases of a new flare, the dose was increased by 500 mg/week up to 3 g/day

Usual Pediatric Dose

Ulcerative Colitis

6 years or older

Initial therapy: 40 to 60 mg/kg/day orally divided into 3 to 6 doses
Maintenance therapy: 30 mg/kg/day orally divided into 4 doses

Juvenile Rheumatoid Arthritis

6 years or older: 30 to 50 mg/kg/day orally in 2 equally divided doses
Maximum dose: 2 g/day (normally)

Side Effects of Sulfasalazine

The most common

stomach pain, especially if it comes along with fever and diarrhea or constipation
yellowing of the skin or eyes
loss of appetite
Constipation
sleepiness or unusual drowsiness
clumsiness or unsteadiness
dizziness
drowsiness
dry mouth
false sense of well-being
increased watering of mouth
lightheadedness
constipation;
vision changes;
breast swelling (in men or women); or
decreased sex drive, impotence, or difficulty having an orgasm.
blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
restless muscle movements in your eyes, tongue, jaw, or neck;

Common

Drowsiness and lightheadedness the day after taking the medicine.
Confusion.
Numbed emotions.
Visual disturbances such as blurred vision or double vision.
Shaky movements and unsteady walk (ataxia).
Loss of memory (amnesia).
Muscle weakness.
Dizziness.
A headache.
Skin rashes.
Disturbances of the gut such as diarrhea, c onstipation, nausea, vomiting or abdominal pain.
Difficulty in passing urine (urinary retention).
Changes in sex drive.
Low blood pressure (hypotension).
Blood disorders.
Jaundice.
Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
Nightmares or hallucinations (tell your doctor if you experience this).

Rare

agitation
anxiety
behavioural changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
confusion
increased trouble sleeping
memory problems
muscle spasms
shortness of breath

Drug Interactions of Sulfasalazine

Sulfasalazine may interact with following drugs, supplyments, & may change the efficacy of drugs

abatacept
anakinra
anti-tumour necrosis factor agents (e.g., adalimumab, etanercept, infliximab, )
azathioprine
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
beta-blockers (e.g., carvedilol, metoprolol, propranolol)
carbamazepine
clonidine
clozapine
corticosteroids (e.g.dexamethasone, hydrocortisone, prednisone)
cyclosporine
diltiazem
imatinib
macrolide antibiotics (e.g., clarithromycin, erythromycin)
methotrexate
methyldopa
mycophenolate
phenobarbital
phenytoin
rituximab
tacrolimus
verapamil

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Pregnancy & Lactation of Sulfasalazine

FDA Pregnancy Category B

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication passes into breast milk. If you are a breastfeeding mother and are taking sulfasalazine, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. This medication is not recommended for children with juvenile rheumatoid arthritis.