Sirolimus (Rapamycin) CAS
No: 53123-88-9 Description of Sirolimus: Antibiotic which demonstrates
immunosuppressive properties. It has been shown to block T-cell activation
and proliferation, as well as, the activation of p70 S6 kinase. Also
anti-inflammatory. Name derived from the native word for Easter Island,
Rapi Nui. Chemical Formula: C51H79NO13 Proper
Use of Sirolimus:
Molecular Weight: M.W. 914.2
Solubility: Soluble in DMSO and Methanol.
Boiling Point / Melting Point: BP/MP: 182-186＜C
Appearance: Yellow Solid
Take Sirolimus only as directed by your doctor. Do not use more or less of it, and do not use it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out. Using too much will increase the risk of side effects, while using too little may lead to rejection of your transplanted kidney.
To help you remember to take your medicine, try to get into the habit of taking it at the same time each day. This will help sirolimus work better by keeping a constant amount in the blood.
Absorption of this medicine may be changed if you change your diet. This medicine should be taken consistently with respect to meals. You should not change the type or amount of food you eat unless you discuss it with your health care professional.
Do not stop taking this medicine without first checking with your doctor. You may have to take this medicine for the rest of your life to prevent your body from rejecting the transplant.
Sirolimus usually is used along with a corticosteroid (cortisone-like medicine) and cyclosporine (another immunosuppressive agent). Sirolimus should be taken 4 hours after cyclosporine modified oral solution (Neoral ) or cyclosporine modified capsules (Neoral). If you have any questions about this, ask your health care professional.
Mix sirolimus oral solution with at least 2 ounces (1/4 cup, 60 milliliters [mL]) of water or orange juice in a glass or plastic container. Stir the mixture well and drink it immediately. Then, rinse the container with at least 4 ounces (1/2 cup, 120 mL) of additional water or orange juice, stir it well, and drink it to make sure that all of the medicine is taken.
Check with your doctor before you stop using cyclosporine when you have been taking sirolimus together with cyclosporine for 4 months after your transplant. Your doctor will tell you if you need to keep taking cyclosporine.
Dosing?
The dose of sirolimus will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of sirolimus. If your dose is different, do not change it unless your doctor tells you to do so. If you have any questions about the proper dose of sirolimus, ask your doctor.
For oral dosage
form (oral solution or tablets):
Adults and children 13 years of age and older weighing 88 pounds (40
kilograms) or more: The usual dose is 2 milligrams (mg) a day after
an initial one-time dose of 6 mg.
For children 13 years of age and older who weigh less than 88 pounds
(40 kilograms): The dose is based on body size. It is usually 1 mg
per square meter of body surface area once a day after an initial
one-time dose of 3 mg per square meter of body surface area.
For children up to 13 years of age: Use and dose must be determined
by your doctor.
Missed dose of Sirolimus:
If you miss a dose of sirolimus and remember it within 12 hours, take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose, go back to your regular dosing schedule, and check with your doctor. Do not double doses.
Storage:
To store Sirolimus:
Keep out of the
reach of children.
Store the oral liquid form in the refrigerator.
Store tablets at room temperature.
Protect from exposure to light.
Keep the medicine from freezing.
Do not keep outdated medicine or medicine no longer needed. Ask your
health care professional how you should dispose of any medicine you
do not use. Be sure that any discarded medicine is out of the reach
of children.
Precautions While Using Sirolimus:
It is very important that your doctor check your progress at regular
visits to make sure that this medicine is working properly and to
check for unwanted effects.
While you are taking sirolimus, it is important to maintain good dental hygiene and see a dentist regularly for teeth cleaning.
Raw oysters or other shellfish may contain bacteria that can cause serious illness and possibly death. This is more likely to be a problem if these foods are eaten by patients with certain medical conditions. Even eating oysters from ＾clean￣ water or good restaurants does not guarantee that the oysters do not contain the bacteria. Eating raw shellfish is not a problem for most healthy people; however, patients with the following conditions may be at greater risk: cancer, immune disorders, organ transplantation, long-term corticosteroid use (as for asthma, arthritis, or organ transplantation), liver disease (including viral hepatitis), excess alcohol intake (2 to 3 drinks or more per day), diabetes, stomach problems (including stomach surgery and low stomach acid), and hemochromatosis (an iron disorder). Do not eat raw oysters or other shellfish while you are taking sirolimus. Be sure oysters and shellfish are fully cooked.
While you are being treated with sirolimus, and after you stop treatment with it, it is important to see your doctor about the immunizations (vaccinations) you should receive. Do not get any immunizations without your doctor's approval. Sirolimus may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your household should not take or have recently taken oral polio vaccine since there is a chance they could pass the polio virus on to you. Also, avoid other persons who have taken the oral polio vaccine. Do not get close to them, and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.
Treatment with sirolimus may also increase the chance of getting other infections. If you can, avoid people with colds or other infections. If you think you are getting a cold or other infection, check with your doctor.
Grapefruits and grapefruit juice may increase the effects of sirolimus by increasing the amount of this medicine in your body. You should not eat grapefruit or drink grapefruit juice while you taking this medicine.
Sirolimus may cause you to have a greater risk for getting skin cancer. When you begin taking this medicine:
，Stay out
of direct sunlight, especially between the hours of 10:00 a.m. and
3:00 p.m., if possible.
，Wear protective clothing, including a hat. Also, wear sunglasses
，Apply a sun block product that has a skin protection factor
(SPF) of at least 15. Some patients may require a product with a higher
SPF number, especially if they have a fair complexion. If you have
any questions about this, check with your health care professional.
，Apply a sun block lipstick that has an SPF of at least 15
to protect your lips
，Do not use a sunlamp or tanning bed or booth.
，Check with your doctor right away if you notice a new mole;
a change in size, shape or color of an existing mole; or a mole that
leaks fluid or bleeds.
Side Effects of Sirolimus:
Along with the needed effects of sirolimus, a medicine may cause some
unwanted effects. Although not all of these side effects may occur,
if they do occur they may need medical attention.
Also, because of the way sirolimus acts on the body, there is a chance that it may cause effects that may not occur until years after the medicine is used. These delayed effects of taking siroimus may include certain types of cancer, such as lymphoma.
Check with your doctor or nurse immediately if any of the following side effects occur after you taking sirolimus:
More common
，Black or red, tarry stools; chest pain ; general feeling of
discomfort or illness; shortness of breath; swollen glands ; weight
loss, unusual; yellow skin and eyes
Check with your doctor as soon as possible if any of the following
side effects occur after you taking sirolimus.:
More common
，Abdominal cramps or pain; accumulation of pus; anxiousness,
unexplained; backache; bleeding from gums or nose; blindness; bloody
or cloudy urine; blue lips and fingernails; blurred vision ; body
aches or pain; bone pain; bruising; burning while urinating; burning,
dry, or itching eyes; burning or stinging of skin; burning, tingling,
numbness, or pain in the hands, arms, feet, or legs; change in mental
status; changes in skin color; chills; cold hands and feet; cold sweats;
confusion; convulsions (seizures); cough; cough producing mucus; cough
that sometimes produces a pink frothy sputum; coughing up blood; dark
or bloody urine; deafness; decreased urge to urinate; decreased urine
output ; decreased vision; difficult, fast, noisy breathing sometimes
with wheezing; difficulty in breathing or swallowing; difficulty speaking;
dilated neck veins; discharge from eye ; dizziness; drowsiness ; dry
mouth; ear congestion ; earache; excessive tearing ; extreme fatigue;
eye pain ; facial hair growth in females; fainting; faintness or lightheadedness
when getting up from lying or sitting position; fast, slow, or irregular
heartbeat; fatigue; feeling faint; feeling of warmth or heat; fever;
flushed, dry skin; flushing or redness of skin, especially on face
and neck; fractures; frequent urge to urinate ; fruit-like breath
odor; full or round face, neck, or trunk; increased menstrual flow
or vaginal bleeding; increased hunger; increased sweating; increased
thirst ; increased urination; irregular breathing; irritability; itching,
pain, redness, swelling, tenderness, warmth on skin; lab results that
show problems with liver; large, flat, blue or purplish patches in
the skin; lightheadedness; lack or loss of appetite; loss of consciousness;
loss of sexual ability, desire, drive, or performance; loss of voice
; lower back or side pain; lower back or side pain; lump in abdomen;
menstrual irregularities; mood changes ; muscle cramps in hands, arms,
feet, legs, or face ; muscle pain; muscle wasting ; nasal congestion;
nausea or vomiting; noisy breathing; numbness or tingling around lips,
hands, or feet; pain in chest, groin, or legs, especially the calves;
pain, tenderness, swelling of foot or leg; painful blisters on trunk
of body; painful cold sores or blisters on lips, nose, eyes, or genitals;
painful or difficult urination; pale skin; paralysis; pinpoint red
spots on skin; pounding or racing heartbeat or pulse; prolonged bleeding
from cuts; pus in urine; rapid heartbeat; rapid, shallow breathing
; rash; red or dark brown urine; redness or swelling in ear; redness,
pain, swelling of eye, eyelid, or inner lining of eyelid; ringing
in the ears; runny nose; sensation of pins and needles; severe constipation;
severe vomiting; severe, sudden headache; slurred speech; sneezing;
sore mouth or tongue; sore throat; sores or white spots on lips or
in mouth; stabbing pain; stomach pain or upset; stomachache; sudden
decrease in amount of urine; sudden loss of coordination; sudden,
severe weakness or numbness in arm or leg; sudden, unexplained shortness
of breath; sweating; swelling of face, fingers, hands, ankles, feet,
or lower legs; swollen glands; swollen, painful or tender lymph glands
in neck, armpit, or groin; swollen, red, tender area of infection;
tenderness, pain, swelling, warmth, skin discoloration, and prominent
superficial veins over affected area; tightness in chest; tiredness;
tremor; trouble breathing; ulcers on lips or in mouth; unusual bleeding
or bruising; unusual tiredness or weakness ; vision changes; weakness
; weakness or heaviness of legs; weight gain; wheezing; white patches
in mouth and/or on tongue
Less common
Bloating; change is size, shape or color of existing mole; darkened
urine; hoarseness; mole that leaks fluid or bleeds; new mole; pains
in stomach, side or abdomen, possibly radiating to the back; skin
ulcer or sores
Rare
Weight gain, unusual
Unknown frequency
Abnormal wound healing; hives; itching; puffiness or swelling of the
eyelids or around the eyes, face, lips, or tongue
Other side effects of taking sirolimus may occur that usually do not
need medical attention. These side effects may go away during treatment
as your body adjusts to the medicine. However, check with your doctor
if any of the following side effects continue or are bothersome:
More common
Abdomen enlarged; abnormal vision; acne; belching; blistering, crusting,
irritation, itching, or reddening of skin; bloated full feeling; burning
feeling in chest or stomach; burning, crawling, itching, numbness,
prickling, "pins and needles" or tingling feeling; constipation;
continuing ring or buzzing or other unexplained noise in ears; cracked,
dry, scaly skin; crying; decrease in frequency of urination; decrease
in height; decreased interest in sexual intercourse; degenerative
disease of the joint; depersonalization ; diarrhea; difficulty in
moving; difficulty in passing urine [dribbling]; discouragement; dysphoria;
ear pain; euphoria; excess air or gas in stomach or intestines; excessive
muscle tone, muscle tension or tightness; fear; feeling sad or empty;
headache; hearing loss; heartburn; inability to have or keep an erection;
increase in heart rate; increased hair growth, especially on the face;
increased urge to urinate during the night; indigestion; irritation
in mouth; itching skin; joint pain or swelling; kidney pain; leg cramps;
loss of bladder control ; loss of energy or weakness; loss of interest
or pleasure; loss of strength or energy; lower abdominal pain; mental
depression; muscle aches, pain, stiffness, or weakness; nervousness;
pain; pain in back, ribs, arms, or legs; pain or burning in throat;
pain or tenderness around eyes and cheekbones; paranoia; passing gas;
pelvic pain; quick to react or overreact emotionally; rapid breathing;
rapidly changing moods; inflammation, redness, or swelling of gums
or mouth; shaking or trembling; shivering; sleepiness; sunken eyes;
swelling; swelling of the scrotum; tender, or enlarged gums; tenderness
in stomach area; thickening of the skin; trouble concentrating; trouble
in sleeping ; waking to urinate at night; wrinkled skin.
Other side effects not listed above of sirolimus may also occur in
some patients. If you notice any other effects after you take sirolimus,
check with your doctor.
