Generic Pentasa

MESALAMINE (5-AMINOSALICYLIC ACID, 5-ASA)
Tablets, delayed release: 400 mg (Rx) Asacol (Procter & Gamble)
Capsules, controlled release: 250 mg (Rx) Pentasa (Aventis)
Suppositories: 500 mg (Rx) Rowasa (Solvay)
Rectal suspension: 4 g/60 mL (Rx) Rowasa (Solvay)

Indications
Chronic inflammatory bowel disease:
Ural - Remission and treatment of mildly to moderately active ulcerative colitis.
Rectal - Treatment of active mild to moderate distal ulcerative colitis, proctosigmoiditis, or proctitis.

Administration and Dosage
Oral:
Tablets - 800 mg 3 times daily for a total dose of 2.4 g/day for 6 weeks.
Capsules - 1 g 4 times daily for a total dose of 4 g for up to 8 weeks.
Suppository: One suppository (500 mg) 2 times daily. Retain the suppository in the rectum for 1 to 3 hours or more if possible to achieve maximum benefit. While the effect may be seen within 3 to 21 days, the usual course of therapy is 3 to 6 weeks depending on symptoms and sigmoidoscopic findings. Suspension: The usual dosage of mesalamine suspension enema in 60 mL units is 1 rectal instillation (4 g) once a day, preferably at bedtime, and retained for approximately 8 hours. While the effect may be seen within 3 to 21 days, the usual course of therapy is 3 to 6 weeks depending on symptoms and sigmoidoscopic findings.

Actions
Pharmacology: Sulfasalazine is split by bacterial action in the colon into sulfapyridine and mesalamine (5-ASA).
The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical father than systemic, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
Pharmacokinetics:
Absorption/Distribution -
Rectal: Mesalamine administered rectally as a suspension enema is poorly absorbed from the colon and is excreted principally in the feces during subsequent bowel movements. At steady state, about 10% to 30% of the daily 4 g dose can be recovered in cumulative 24 hour urine collections.
Oral:
Tablets - Mesalamine tablets are coated with an acrylic-based resin that delays release of mesalamine until it reaches the terminal ileum and beyond. Approximately 28% is absorbed after oral ingestion, leaving the remainder available for topical action and excretion in the feces. Mesalamine from oral mesalamine tablets appears to be more extensively absorbed than that released from sulfasalazine.
Capsules - Mesalamine capsules are designed to release therapeutic quantities of the drug throughout the GI tract; 20% to 30% of mesalamine is absorbed. Plasma mesalamine concentration peaked at about 1 mcg/mL 3 hours after administration of a 1 g dose and declined in a biphasic manner. Mean terminal half-life was 42 minutes after IV administration. Metabolism/Excretion -
Rectal: Whatever the metabolic site, most absorbed mesalamine is excreted in urine as the N-acetyl-5-ASA metabolite. While the elimination half-life of mesalamine is short (0.5 to 1.5 hours), the acetylated metabolite exhibits a half-life of 5 to 10 hours.
Oral:
Tablets - Following oral administration, the absorbed mesalamine is rapidly acetylated in the gut mucosal wall and by the liver. It is excreted mainly by the kidneys as N-acetyl-5-ASA. The half-lives of elimination for mesalamine and the metabolite are usually approximately 12 hours, but ate variable ranging from 2 to 15 hours.
Capsules - Elimination of free mesalamine and salicylates in feces increased proportionately with the dose. N-acetyl-5-ASA was the primary compound excreted in the urine (19% to 30%).

Contraindications
Hypersensitivity to mesalamine, salicylates, or any component of the formulation.

Warnings
Intolerance/Colitis exacerbation: Mesalamine has been implicated in the production of an acute intolerance syndrome or exacerbation of colitis characterized by cramping, acute abdominal pain and bloody diarrhea, and occasionally fever, headache, malaise, pruritus, conjunctivitis, and rash. Symptoms usually abate when mesalamine is discontinued.
Pancolitis: While using mesalamine, some patients have developed pancolitis.
Hypersensitivity reactions: Most patients who were hypersensitive to sulfasalazine were able to take mesalamine enemas without evidence of any allergic reaction. Nevertheless, exercise caution when mesalamine is initially used in patients known to be allergic to sulfasalazine.
Renal function impairment: Renal impairment, including minimal change nephropathy, and acute and chronic interstitial nephritis, has occurred.
Pregnancy: Category B. Mesalamine is known to cross the placental barrier.
Lactation: Low concentrations of mesalamine and higher concentrations of N-acetyl-5-ASA have been detected in breast milk.
Children: Safety and efficacy for use in children have not been established.

Precautions
Pericarditis: Pericarditis has occurred rarely with mesalamine-containing products including sulfasalazine.

Adverse Reactions
Adverse reactions may include abdominal pain/cramps/discomfort; colitis exacerbation; constipation; diarrhea; dyspepesia; eructation; flatulence/gas; nausea; vomiting; asthenia; chills; dizziness; fever; headache; malaise/fatigue/weakness; sweating; pharyngitis; rhinitis; pruritus; rash/spots; arthralgia; hack pain; hypertonia; myalgia; chest pain; dysmenorrhea; edema; flu syndrome; pain.
GASTROINTESTINAL

EMOTIONAL HEALTH: THE FEELING YOU
The term emotional health is often used interchangeably with mental health. Although emotional and mental health are closely intertwined, emotional health more accurately refers to the "feeling," or subjective, side of psychosocial health. Emotions are intensified feelings or complex patterns of feelings that we experience on a minute-by-minute, day-to-day basis. Loving, caring, hating, hurt, despair, release, joy, anxiety, fear, frustration, and intense anger are some of the many emotions we experience. Typically, emotions are described as the interplay of four components: physiological arousal, feelings, cognitive (thought) processes, and behavioral reactions. Each time you are put in a stressful situation, you react physiologically while your mind tries to sort things out. You consciously or unconsciously react based on how rationally you interpret the situation.
Psychologist Richard Lazarus has indicated that there are four basic types of emotions: (1) emotions resulting from harm, loss, or threats; (2) emotions resulting from benefits; borderline emotions, such as hope and compassion; and more complex emotions, such as grief, disappointment bewilderment, and curiosity. Each of us may experience of these emotions in any combination at any time. As rational beings, it is our responsibility to evaluate our individual emotional responses, the environment that is causing these responses, and the appropriateness of our actions.
Emotionally healthy people are usually able to respond in an appropriate manner to upsetting events. When they feel threatened, they are not likely to react in an extreme fashion, behave inconsistently, or adopt an offensive attack mode.
Even when their feelings are trampled upon or they suffer agonizing pain because of a lost love, they keep their emotions in check.
Emotionally unhealthy people are much more likely to let their feelings overpower them than are emotionally healthy people. Emotionally unhealthy people may be highly volatile and prone to unpredictable emotional outbursts and to inappropriate, sometimes frightening responses to events. An ex-boyfriend who becomes so angry that he begins to hit you and push you around in front of your friends because he is jealous of your new relationship is showing an extremely unhealthy and dangerous emotional reaction. Such violent responses have become a problem of epidemic proportions in the United States.
Emotional health also affects social health. Someone feeling hostile or withdrawn or displaying other mood fluctuations may be avoided by others. People in the midst of emotional turmoil may be grumpy, nasty, irritable, or overly quiet; they may cry easily or demonstrate other disturbing emotional responses. Since they are not much fun to be around, their friends may avoid them at the very time they are most in need of emotional support. Social isolation is just one of the many potential negative consequences of unstable emotional responses.
For students, a more immediate concern is the impact of emotional trauma or turmoil on academic performance. Have you ever tried to study for an exam after a fight with a close friend or family member? Emotional turmoil may seriously affect your ability to think, reason, or act in a rational way. Many otherwise rational, mentally healthy people do ridiculous things when they are going through a major emotional upset. Mental functioning and emotional responses are indeed intricately connected.
*28/277/5*
GENERAL HEALTH

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