Pain in elderly people – Pamelor

Complaints of pain observed in 25% – 50% of elderly people living at home and from 45% to 80% living in institutions in which they are given a long uhod.1-6 untreated pain has serious consequences, which include depression, decreased socialization, sleep disturbance , violation of legal capacity, slowing recovery and rising health care costs. / 3,7,8 /.
Recommendations for survey
Although patients aged 60-70 years are able to report and assess signs of pain, but evaluation of pain in patients most venerable age may be complicated by their complex conditions and situations. Complicated circumstances include loss of vision and hearing, cognitive disturbances associated with delirium, dementia and other neurological diseases, cultural barriers and false belief, such as the fact that pain is an inevitable part of aging. / 2,7,9-12 /
In the past ten years there have been several studies that have been devoted to assessing the best ways to assess pain in elderly lyudey/.10-14 / / Many of the elderly did not accurately respond to questions about pain. However, the elderly with impaired cognitive abilities and skills, disorganized speech, have difficulty in describing their discomfort and may be unable to comprehend the agonizing pain, which prevents obsledovaniyu.7, 9,11,13 In one study of elderly patients with hip fracture who were violated the cognitive and verbal skills, have difficulties with the localization of pain and said that they “hurt everywhere.” “15 In other cases, the patients experienced pain and discomfort, but a negative answer to a question regarding boli.15 However, compared with controls, they are equally likely to report the presence of pain,” yes “or” no. “
The key to optimal treatment is the identification of pain. Health workers and staff should use the pain assessment tools that are simple, easily accessible, printed big and bold letters and in a language that patients understand / 12,14,16 /. We recommend using a verbal descriptive scale (The Verbal Descriptor Scale – VDS) because it uses the familiar words (slight pain, mild pain, moderate pain, severe pain, extreme pain and the pain is so strong as it can be) / .14 /. In two studies, the scale was considered the preferred and most easily understood by the elderly in communities / 15 /. In addition, she was seen approximately 73% of hospitalized older people with cognitive disabilities vozmozhnostyami/.15.
Recommendations of the American Geriatric Society (American Geriatric Society – AGS) also recommend the use of synonyms pain: pain, pressure, burning, lumbagos, compression, inflammation, neudobstvo.16 Studies have shown that, despite the fact that the visual analogue scale (Visual Analog Scales – VAS) and categorical scale (such as VDS) is closely correlated with each other, there is wide variation in VAS responses for each category and the overlap between the categories of indicators / 14 /.
Were developed some new methods of examination have not spoken to and severely damaged starikov/11 ,13,17-21. These methods include general observation which drew attention to the following behavior: movement of persons (faces, nahmurivanie, inflating the cheeks), specific of the body (grinding, fixing, obereganie, dotragivanie) and voice (cries, screams, cries) / 11,13,17-21 /. The researchers encourage the documentation of other forms of pain: poor appetite, depressive symptoms, sleep disturbances, functional disability, agitated behavior, resisting care, rejecting behavior and crying. / 9,11,13,17 /
Since the elderly with cognitive impairment can forget about the pain, if they are sitting quietly, a good strategy is to check during the movement and palpirovanie suspicious oblasti/21, 22. Consult with your family on the patient’s previous history of pain and use of analgesics / 15,21 / /
Older people with impaired cognition, aggressive or agitated behavior and resistance to care may be associated with untreated pain / 21-24 /. Preliminary study of aggressive elderly with cognitive impairment document the level of aggression are greatly increased in subjects diagnosed with arthritis or those who have two or more of diagnosis, which can cause boli/21. New behavioral changes in patients with dementia may signal that many medical problems, including urinary tract infections, constipation, changes in the heart and discomfort as a result of falls or injuries. Pilot studies empirical application of pain medication to reduce the aggressiveness yielded some success. These studies showed that treatment of pain can reduce the use of tranquilizers prescribed for the treatment of aggressive behavior / 23,24 /.
Recommendations for treatment
American Gerontological Society has published practical recommendations for the treatment of chronic pain in older people 1998 / 16 /. Some psychological changes with aging affect the treatment of chronic pain in the elderly, frail patients. These features include slow absorption of medications, metabolic disorders and processes of elimination. These features create problems associated with excessive sedation, disorientation, constipation and urinary retention / 16,25,26 /.
American Medical Directors Association (American Medical Directors Association-AMDA) in 1999 published guidelines for the treatment of chronic pain in older / 25 /. These recommendations promote the following principles of treatment of pain:
To the extent possible, use the least invasive (oral) route destination analgesics.
Identifying the causes of pain is necessary to select the best.
Cautious approach would help avoid having excessive sedation / 26 /.
The principles of the recommendations of the AGS and AMDA introduced by discussing the following circumstances.
Short-acting Analgesics are good for acute illness or sudden acute exacerbation of chronic illness. Atsetoaminofen drug of choice to alleviate the acute and moderate pain. Regularly appointed atsetoaminofen more effective than if he is appointed as needed. Often the elderly come to the nurse practitioner, complaining of pain, but they have not tried the application atsetoaminofena in a dose of 325 mg. Patients who say atsetoaminofen “not working” should be encouraged to use the dose from 650 mg to 1,000 mg three – four times a day, if they do not have a history of alcoholism or liver disease.
The daily prescription medications can be “ahead of” the emergence of problems with pain and maintain functional activity. Keep in mind the empirical purpose of pain therapy for deeply affected, being home patients who are experiencing pain and asking for help / 23,24 /. If we take comfort main objective empirical therapy will help achieve this goal. In one study testing atsetoaminofena at a dose of 650 mg three times daily for 10 home residents with difficulties in behavior led to a 63% reduction of behavioral symptoms / 24 /.
The dose of acetaminophen should not exceed 4 grams in 24 hours. This threshold can be easily exceeded if the drug is given as needed. Keep in mind the differences in dosages of acetaminophen in combined acetaminophen-opioid drugs. For example, acetaminophen with codeine (Tylenol # 3) contains 325 mg of acetaminophen, 1 tablet, oxycodone (oxycodone) acetaminophen (Percocet) and hydrocodone (hydrocodone) and acetaminophen (Vicoden) contains 500 mg and propoxyphene napsylate with acetaminophen (Darvocet N100) contains 650 mg of acetaminophen in 1 tablet.
NSAIDs (Nonsteroidal antiinflammatory drugs-NSAID) to be appointed by the elderly with care, especially with regard to patients with impaired renal function receiving anticoagulation therapy and bleeding in anamneze/16. Recommendations AGS advised to avoid long-term use of any NSAID, especially in high doses and in the form of long-acting drugs (such as naproxen sodium; Naprosyn, Aleve) due to increased risk of gastric ulcer bleeding / 16 /. Assign short-drugs (eg ibuprofen) in small doses (400 mg) for adults who require nonsteroidal anti-inflammatory preparaty/26. The medicine should be taken with meals, and course of treatment should be short-lived / 26 /.
Recommendations AGS warn against the simultaneous appointment of more than one NSAID. With extreme caution should be used NSAID in patients who take oral corticosteroids. Some observations indicate that the 14-day course of 400 mg of ibuprofen brings a more significant relief and improve function in elderly osteoarthritis knee or bedra/27. Such a short course of treatment may be useful in exacerbations of arthritis. However, prolonged treatment at high doses can lead to swelling of the lower limbs, gastric bleeding and renal dysfunction / 26 /.
The recent removal of rofecoxib from the market (rofecoxib-Vioxx) due to increased risk of cardiovascular episodes, as well as similar questions about other COX-2 inhibitors, confirms the need to avoid their use in the elderly / 28 /. This group of drugs inhibits the production of prostaglandins associated with inflammation and gives fewer gastrointestinal adverse reactions than the older pain relievers / 25,28 /. Nephrotoxicity, hypertension, and edema – the usual side effects of NSAID and they also are associated with COX-2 inhibitor. In determining the dosage of NSAID in the elderly should monitor renal function.
Opioid analgesic drugs (morphine, codeine, gidromorfan, hydrocodone, oxycodone) are useful for relief of moderate to severe pain. Unlike atsetoaminofena, opioid funds may titrate doses to achieve the effect, if they are not part of the combined drugs. However, the combination drugs that include atsetoaminofen have a limit as the limit “ceiling” dose of acetaminophen is 4 grams per day. Opioid funds available in the form of many drugs. Selecting the drug depends largely on the strength of pain, medical and cognitive status and tolerance to side effects / 16,25,26 /.
Continuing pain should be treated dlitelnodeystvuyuschimi or slow to eliminate drugs. Slow to eliminate drugs should be appointed at the initial high doses and should not be appointed opioid “naive” patients. Routine doses of drugs to titrate short-range, rising and allowing the patient to move to a long-acting drugs. Requires a good understanding of morphine equivalency. For example, a dose of 5 mg of liquid concentrate of morphine every 4 – 6 hours will be “ekvianalgetichna” one dose of oxycodone (oxycodone) and hydrocodone-atseaminofen (hydrocodone-acetaminophen) tablet over the same intervals.
The dose of morphine can concentrate stepwise increase to obtain relief.
However, side effects such as constipation, sedation, violations of recognition and instability when walking can be a contraindication to achieve the necessary dosage for pain relief / 25,26 /. Start with a low dose and gradually increase to track the side effects. Constipation can be combated with the help of laxatives. A simple approach such as the appointment of cherry flavored liquid acetaminophen (which can cause diarrhea), with oral morphine concentrate (which causes constipation) opens the way to balance the side effects of the assignment anlgetikov central and peripheral deystviya.15
Neuropathic pain is often described as “shooting” and the searing pain.
Tricyclic antidepressants (nortriptyline [Pamelor], desipramine (desipramine 0 [Norpramin]) and proivosudorozhnye drugs gabapentin – (gabapentin 0 [Neurontin]) in general are most effective for treating this type of pain than traditional pain relievers. Gabapentin (Gabapentin) may be effective for reduce neuropathic cancer pain in patients who receive treatment opioidami./29 / Gabapentin has a low profile of side effects, unlike the high-profile in anticholinergic tricyclic antidepressants (which can increase levels of anxiety and confusion in patients with mild dementia with). Recommendations AGS advised to apply carbamazepine (carbamazepine – Tegretol) in trigeminal neuralgia / 16,26 / /
By achieving comfort
Pain is a frustrating (frustrating) problem for the elderly and infirm patients. The combination of routine use of drugs, careful monitoring and additional non-pharmacological approaches recommended in order to achieve that sense of comfort for the patient.

Complaints of pain observed in 25% – 50% of elderly people living at home and from 45% to 80% living in institutions in which they are given a long uhod.1-6 untreated pain has serious consequences, which include depression, decreased socialization, sleep disturbance , violation of legal capacity, slowing recovery and rising health care costs. / 3,7,8 /.

Recommendations for survey

Although patients aged 60-70 years are able to report and assess signs of pain, but evaluation of pain in patients most venerable age may be complicated by their complex conditions and situations. Complicated circumstances include loss of vision and hearing, cognitive disturbances associated with delirium, dementia and other neurological diseases, cultural barriers and false belief, such as the fact that pain is an inevitable part of aging. / 2,7,9-12 /

In the past ten years there have been several studies that have been devoted to assessing the best ways to assess pain in elderly lyudey/.10-14 / / Many of the elderly did not accurately respond to questions about pain. However, the elderly with impaired cognitive abilities and skills, disorganized speech, have difficulty in describing their discomfort and may be unable to comprehend the agonizing pain, which prevents obsledovaniyu.7, 9,11,13 In one study of elderly patients with hip fracture who were violated the cognitive and verbal skills, have difficulties with the localization of pain and said that they “hurt everywhere.” “15 In other cases, the patients experienced pain and discomfort, but a negative answer to a question regarding boli.15 However, compared with controls, they are equally likely to report the presence of pain,” yes “or” no. ”

The key to optimal treatment is the identification of pain. Health workers and staff should use the pain assessment tools that are simple, easily accessible, printed big and bold letters and in a language that patients understand / 12,14,16 /. We recommend using a verbal descriptive scale (The Verbal Descriptor Scale – VDS) because it uses the familiar words (slight pain, mild pain, moderate pain, severe pain, extreme pain and the pain is so strong as it can be) / .14 /. In two studies, the scale was considered the preferred and most easily understood by the elderly in communities / 15 /. In addition, she was seen approximately 73% of hospitalized older people with cognitive disabilities vozmozhnostyami/.15.

Recommendations of the American Geriatric Society (American Geriatric Society – AGS) also recommend the use of synonyms pain: pain, pressure, burning, lumbagos, compression, inflammation, neudobstvo.16 Studies have shown that, despite the fact that the visual analogue scale (Visual Analog Scales – VAS) and categorical scale (such as VDS) is closely correlated with each other, there is wide variation in VAS responses for each category and the overlap between the categories of indicators / 14 /.

Were developed some new methods of examination have not spoken to and severely damaged starikov/11 ,13,17-21. These methods include general observation which drew attention to the following behavior: movement of persons (faces, nahmurivanie, inflating the cheeks), specific of the body (grinding, fixing, obereganie, dotragivanie) and voice (cries, screams, cries) / 11,13,17-21 /. The researchers encourage the documentation of other forms of pain: poor appetite, depressive symptoms, sleep disturbances, functional disability, agitated behavior, resisting care, rejecting behavior and crying. / 9,11,13,17 /

Since the elderly with cognitive impairment can forget about the pain, if they are sitting quietly, a good strategy is to check during the movement and palpirovanie suspicious oblasti/21, 22. Consult with your family on the patient’s previous history of pain and use of analgesics / 15,21 / /

Older people with impaired cognition, aggressive or agitated behavior and resistance to care may be associated with untreated pain / 21-24 /. Preliminary study of aggressive elderly with cognitive impairment document the level of aggression are greatly increased in subjects diagnosed with arthritis or those who have two or more of diagnosis, which can cause boli/21. New behavioral changes in patients with dementia may signal that many medical problems, including urinary tract infections, constipation, changes in the heart and discomfort as a result of falls or injuries. Pilot studies empirical application of pain medication to reduce the aggressiveness yielded some success. These studies showed that treatment of pain can reduce the use of tranquilizers prescribed for the treatment of aggressive behavior / 23,24 /.

Recommendations for treatment

American Gerontological Society has published practical recommendations for the treatment of chronic pain in older people 1998 / 16 /. Some psychological changes with aging affect the treatment of chronic pain in the elderly, frail patients. These features include slow absorption of medications, metabolic disorders and processes of elimination. These features create problems associated with excessive sedation, disorientation, constipation and urinary retention / 16,25,26 /.

American Medical Directors Association (American Medical Directors Association-AMDA) in 1999 published guidelines for the treatment of chronic pain in older / 25 /. These recommendations promote the following principles of treatment of pain:

To the extent possible, use the least invasive (oral) route destination analgesics.

Identifying the causes of pain is necessary to select the best.

Cautious approach would help avoid having excessive sedation / 26 /.

The principles of the recommendations of the AGS and AMDA introduced by discussing the following circumstances.

Short-acting Analgesics are good for acute illness or sudden acute exacerbation of chronic illness. Atsetoaminofen drug of choice to alleviate the acute and moderate pain. Regularly appointed atsetoaminofen more effective than if he is appointed as needed. Often the elderly come to the nurse practitioner, complaining of pain, but they have not tried the application atsetoaminofena in a dose of 325 mg. Patients who say atsetoaminofen “not working” should be encouraged to use the dose from 650 mg to 1,000 mg three – four times a day, if they do not have a history of alcoholism or liver disease.

The daily prescription medications can be “ahead of” the emergence of problems with pain and maintain functional activity. Keep in mind the empirical purpose of pain therapy for deeply affected, being home patients who are experiencing pain and asking for help / 23,24 /. If we take comfort main objective empirical therapy will help achieve this goal. In one study testing atsetoaminofena at a dose of 650 mg three times daily for 10 home residents with difficulties in behavior led to a 63% reduction of behavioral symptoms / 24 /.

The dose of acetaminophen should not exceed 4 grams in 24 hours. This threshold can be easily exceeded if the drug is given as needed. Keep in mind the differences in dosages of acetaminophen in combined acetaminophen-opioid drugs. For example, acetaminophen with codeine (Tylenol # 3) contains 325 mg of acetaminophen, 1 tablet, oxycodone (oxycodone) acetaminophen (Percocet) and hydrocodone (hydrocodone) and acetaminophen (Vicoden) contains 500 mg and propoxyphene napsylate with acetaminophen (Darvocet N100) contains 650 mg of acetaminophen in 1 tablet.

NSAIDs (Nonsteroidal antiinflammatory drugs-NSAID) to be appointed by the elderly with care, especially with regard to patients with impaired renal function receiving anticoagulation therapy and bleeding in anamneze/16. Recommendations AGS advised to avoid long-term use of any NSAID, especially in high doses and in the form of long-acting drugs (such as naproxen sodium; Naprosyn, Aleve) due to increased risk of gastric ulcer bleeding / 16 /. Assign short-drugs (eg ibuprofen) in small doses (400 mg) for adults who require nonsteroidal anti-inflammatory preparaty/26. The medicine should be taken with meals, and course of treatment should be short-lived / 26 /.

Recommendations AGS warn against the simultaneous appointment of more than one NSAID. With extreme caution should be used NSAID in patients who take oral corticosteroids. Some observations indicate that the 14-day course of 400 mg of ibuprofen brings a more significant relief and improve function in elderly osteoarthritis knee or bedra/27. Such a short course of treatment may be useful in exacerbations of arthritis. However, prolonged treatment at high doses can lead to swelling of the lower limbs, gastric bleeding and renal dysfunction / 26 /.

The recent removal of rofecoxib from the market (rofecoxib-Vioxx) due to increased risk of cardiovascular episodes, as well as similar questions about other COX-2 inhibitors, confirms the need to avoid their use in the elderly / 28 /. This group of drugs inhibits the production of prostaglandins associated with inflammation and gives fewer gastrointestinal adverse reactions than the older pain relievers / 25,28 /. Nephrotoxicity, hypertension, and edema – the usual side effects of NSAID and they also are associated with COX-2 inhibitor. In determining the dosage of NSAID in the elderly should monitor renal function.

Opioid analgesic drugs (morphine, codeine, gidromorfan, hydrocodone, oxycodone) are useful for relief of moderate to severe pain. Unlike atsetoaminofena, opioid funds may titrate doses to achieve the effect, if they are not part of the combined drugs. However, the combination drugs that include atsetoaminofen have a limit as the limit “ceiling” dose of acetaminophen is 4 grams per day. Opioid funds available in the form of many drugs. Selecting the drug depends largely on the strength of pain, medical and cognitive status and tolerance to side effects / 16,25,26 /.

Continuing pain should be treated dlitelnodeystvuyuschimi or slow to eliminate drugs. Slow to eliminate drugs should be appointed at the initial high doses and should not be appointed opioid “naive” patients. Routine doses of drugs to titrate short-range, rising and allowing the patient to move to a long-acting drugs. Requires a good understanding of morphine equivalency. For example, a dose of 5 mg of liquid concentrate of morphine every 4 – 6 hours will be “ekvianalgetichna” one dose of oxycodone (oxycodone) and hydrocodone-atseaminofen (hydrocodone-acetaminophen) tablet over the same intervals.

The dose of morphine can concentrate stepwise increase to obtain relief.

However, side effects such as constipation, sedation, violations of recognition and instability when walking can be a contraindication to achieve the necessary dosage for pain relief / 25,26 /. Start with a low dose and gradually increase to track the side effects. Constipation can be combated with the help of laxatives. A simple approach such as the appointment of cherry flavored liquid acetaminophen (which can cause diarrhea), with oral morphine concentrate (which causes constipation) opens the way to balance the side effects of the assignment anlgetikov central and peripheral deystviya.15

Neuropathic pain is often described as “shooting” and the searing pain.

Pamelor

Tricyclic antidepressants (nortriptyline [Pamelor], desipramine (desipramine 0 [Norpramin]) and proivosudorozhnye drugs gabapentin – (gabapentin 0 [Neurontin]) in general are most effective for treating this type of pain than traditional pain relievers. Gabapentin (Gabapentin) may be effective for reduce neuropathic cancer pain in patients who receive treatment opioidami./29 / Gabapentin has a low profile of side effects, unlike the high-profile in anticholinergic tricyclic antidepressants (which can increase levels of anxiety and confusion in patients with mild dementia with). Recommendations AGS advised to apply carbamazepine (carbamazepine – Tegretol) in trigeminal neuralgia / 16,26 / /

By achieving comfort

Pain is a frustrating (frustrating) problem for the elderly and infirm patients. The combination of routine use of drugs, careful monitoring and additional non-pharmacological approaches recommended in order to achieve that sense of comfort for the patient.

January 21, 2010 | Tags: | No Comments »

Arava

Pharmacological action
Base antirheumatic drug. Has antiproliferative, immunomodulatory (immunosuppressive) and anti-inflammatory effect. The active metabolite of leflunomide A771726 inhibits the enzyme degidroorotat dehydrogenase and has an antiproliferative effect. A771726 inhibits in vitro cell proliferation caused by mitogens and DNA synthesis of T-lymphocytes. Antiproliferative activity A771726 seen, apparently at the level of pyrimidine biosynthesis, since the addition of cell culture eliminates the inhibitory effect of uridine metabolite A771726. With the use of radioisotope ligand shown that A771726 selectively binds to the enzyme degidroorotat dehydrogenase, which explains its properties this enzyme and inhibit proliferation of lymphocytes at the stage of G1. Simultaneously A771726 inhibits the expression of receptors for interleukin-2 and core antigen Ki-67 and PCNA, associated with the cell cycle.
Therapeutic effect of leflunomide has been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.
Pharmacokinetics
The absorption and distribution
After oral administration, absorbed 82-95% of the drug. Eating does not affect the absorption leflunamida. Leflunomide is rapidly metabolized with the formation of the active metabolite A771726. Cmax metabolite A771726 determined within 1-24 h after a single dose of the dose. In plasma A771726 rapidly binds to albumin. Untie A771726 fraction is 0.62%. Binding A771726 more variable and somewhat reduced in patients with rheumatoid arthritis or chronic renal insufficiency.
Due to the long T1 / 2 A771726 was used a loading dose of 100 mg for 3 days. Pharmacokinetic parameters A771726 have a linear dependence at doses from 5 mg to 25 mg. In these studies, the clinical effect is closely related to plasma concentration of A771726 and a daily dose of leflunomide. At a dose of 20 mg / day, mean plasma concentration of A771726 at steady-state was 35 micrograms / ml.
Metabolism
Leflunomide is rapidly metabolized in the intestinal wall and liver to one of the main (A771726) metabolite and several secondary metabolites, including 4-trifluorometilalanin. Biotransformation of leflunomide to A771726 and A771726 of the subsequent metabolism are controlled by several enzymes and occur in microsomal and other cell fractions.
Withdrawal
In plasma, urine and feces determined by the trace amounts of leflunomide. Removing A771726 slow and characterized by clearance of 31 mL / h. T1 / 2 – about 2 weeks.
Pharmacokinetics in special clinical cases
Patients on hemodialysis, elimination of the drug quickly and T1 / 2 is shorter.
Data on the pharmacokinetics in patients with liver failure are absent.
Pharmacokinetics in patients younger than 18 years has not been studied.
Elderly patients (65 years and older) pharmacokinetic data correspond approximately to the middle age group.
Indications
- As the reference drug for the treatment of active rheumatoid arthritis to reduce symptoms and delay the development of structural damage of joints.
Dosage regimen
Treatment is initiated with the appointment of a shock dose of 100 mg daily for 3 days. As a maintenance dose prescribed dose of 10 mg to 20 mg 1 time per day.
The therapeutic effect is evident after 4-6 weeks of admission and may grow within 4-6 months.
Tablets should be swallowed whole, drinking plenty of fluids.
Not require dose adjustment for patients older than 65 years.
There are currently no recommendations for dosing regime for patients with mild renal insufficiency.
Side effects
Classification of the alleged frequency of side effects: typical – 1-10%, atypical – 0.1-1%, rare – 0.01-0.1%, very rare – 0.01% or less.
Since the cardiovascular system: typical – increase blood pressure.
From the digestive system: typical – diarrhea, nausea, vomiting, anorexia, lesions of the oral mucosa (thrush, mouth ulceration), abdominal pain, increased hepatic transaminases (particularly ALT, rarely – GGT, alkaline phosphatase, bilirubin); rarely – hepatitis, jaundice, cholestasis, very rarely – liver failure, acute liver necrosis.
On the part of the musculoskeletal system: typical – abscess, atypical – the gap ligaments.
Dermatological reactions: typical – hair loss, eczema, dry skin, atypical – Stevens-Johnson syndrome, Lyell syndrome, erythema multiforme.
The part of the hemopoietic system: typical – leukopenia (white blood cells more 2000/mkl); atypical – anemia, thrombocytopenia (platelets less than 100 000/mkl); rarely – eosinophilia, leukopenia (leukocytes less 2000/mkl), pancytopenia, very rarely – agranulocytosis. The risk of hematologic disorders increases with the recent, concomitant and subsequent application of myelotoxic drugs.
Allergic reactions: typical – rash (including makulo-papular), pruritus; atypical – urticaria; very rare – anaphylactic reactions.
On the part of the exchange processes: hyperlipidemia, hypophosphatemia, reduced levels of uric acid. Laboratory data (not clinically confirmed) showed a modest increase lactate dehydrogenase, creatine phosphokinase.
Other: very rarely – the development of severe infection and sepsis may develop rhinitis, bronchitis and pneumonia. In the application of immunosuppressive drugs increases the risk of cancer and some lymphoproliferative processes.
We can not exclude the possibility of a reversible reduction of sperm concentration, total sperm count and motility.
Contraindications
- Human liver;
- Severe immunodeficiency (including AIDS);
- Pronounced disorders of bone marrow hematopoiesis or anemia, leukopenia, thrombocytopenia due to other causes (other than rheumatoid arthritis);
- Infection heavy flow;
- Moderate or severe renal insufficiency (because of the small experience of clinical observations);
- Severe hypoproteinemia (including with nephrotic syndrome);
- Pregnancy;
- Lactation (breastfeeding);
- Childhood and adolescence to 18 years;
- Hypersensitivity to the ingredients.
The drug is contraindicated in women of childbearing age who do not use adequate contraception.
Pregnancy and lactation
The drug should not be administered during pregnancy and women of childbearing age who are not using reliable contraception. You must verify the absence of pregnancy before starting treatment.
In experimental studies have found that the drug may have fetotoksicheskoe and teratogenic effect.
Patients should be informed that suspected pregnancy should seek medical advice immediately and do a pregnancy test. If the test is positive, the physician should inform the patient about the possible risk to the fetus.
Women who take leflunomide and want to become pregnant (or already in the ensuing pregnancy) procedure is recommended to launch the drug, which will rapidly reduce the concentration of leflunomide and its metabolite in blood plasma (after cessation of treatment prescribed leflunomide kolestiramin in a dose of 8 g 3 times / day within 11 days or 50 g of activated charcoal, crushed into powder, 4 times / day for 11 days).
Next, you need to determine the concentration of metabolite A771726 2 times with an interval of 14 days. From the moment when the concentration of the drug will be fixed below 20 mg / l until fertilization should take 1.5 months.
Note that without the procedure of removing the drug, reduced metabolite concentrations below 20 ug / l occurs in 2 years.
Kolestiramin and activated carbon can affect the absorption of estrogen and progesterone in such a way that reliable oral contraceptives do not guarantee the necessary contraception during launch preparation. It is recommended to use alternative methods of contraception.
Studies in animals have shown that leflunomide or its metabolites are excreted in breast milk milk. Therefore, the need to designate a lactation should resolve the issue of termination of breastfeeding.
There is currently no information confirming the link between taking the drug Arava men and fetotoksicheskim action of the drug. Experimental studies in this direction were made. However, men receiving leflunomide therapy, should be warned of the possible effect of fetotoksicheskom and the need to use adequate contraception. To minimize risk when planning pregnancy should stop taking leflunomide and use kolestiramin to 8 mg 3 times daily for 11 days or 50 grams of powdered activated charcoal 4 times daily for 11 days.
Cautions
Note that the drug Arava may be imposed only after a medical examination (including before starting treatment and during treatment should monitor blood pressure).
Before treatment drug Arava should be mindful of possible increase in the number of side effects in patients previously treated with other basic tools for the treatment of rheumatoid arthritis, which have hepato-and gematotoksicheskim action.
The active metabolite of leflunomide A771726 characterized by long T1 / 2. Therefore, side effects can occur even after cessation of therapy. If you have any similar cases of toxicity or when moving to another base receiving the drug after treatment with leflunomide should be the procedure of removing the drug (after the cessation of leflunomide treatment prescribed kolestiramin in a dose of 8 g 3 times daily for 11 days or 50 g of activated carbon, crushed to powder, 4 times / day for 11 days).
Note that during the development of severe dermatologic adverse reactions, severe infections receiving the drug Arava should stop and immediately initiate the removal of the drug.
Need to monitor patients with tuberculin reactivity due to the risk of activating tuberculosis.
Given the long-term elimination of Arava is not recommended to vaccinate live vaccines against a background of leflunomide treatment.
Overdose
No data on overdose of leflunomide. Admission leflunomide 100 mg daily for 14 days was observed in 10 healthy volunteers. Two of them were removed after a week because of the increased level of transaminases in the blood plasma.
In case of overdose or toxicity is recommended to use kolestiramina or powdered activated carbon. Kolestiramin, take 3 healthy volunteers administered orally to 8 mg 3 times / day during the day, reduced levels of A771726 in plasma by approximately 40% after 24 h and 49-65% after 48 h.
Shown that introduction of activated charcoal orally or via oral gavage (50 mg every 6 hours during the day) reduced the concentration of the active metabolite A771726 in plasma by 37% after 24 h and 48% after 48 h.
Perhaps repetition procedures are preparation for clinical indications.
Drug Interactions
Increased adverse reactions may occur in the case of recent or concomitant use of hepatotoxic drugs or hematotoxicity or when receiving these drugs after starting leflunomide treatment procedure without removing the drug.
Not observed pharmacokinetic interaction between leflunomide (10-20 mg / day) and methotrexate (10-25 mg / week).
Unknown clinically significant interactions with concomitant use of leflunomide and triphasic oral contraceptives, NSAIDs, cimetidine, rifampicin.
Studies in vitro showed that the metabolite of leflunomide A771726 inhibits the activity of cytochrome P450 2C9. Therefore, caution should be prescribed the drug Arava with drugs metabolized by this enzyme system (phenytoin, warfarin, tolbutamide).
Conditions and terms of storage
The product should be stored at temperatures not above 25 ° C. Shelf life – 3 years.
Conditions of supply of pharmacies
The drug is released with a prescription.

Arava

Pharmacological action

Base antirheumatic drug. Has antiproliferative, immunomodulatory (immunosuppressive) and anti-inflammatory effect. The active metabolite of leflunomide A771726 inhibits the enzyme degidroorotat dehydrogenase and has an antiproliferative effect. A771726 inhibits in vitro cell proliferation caused by mitogens and DNA synthesis of T-lymphocytes. Antiproliferative activity A771726 seen, apparently at the level of pyrimidine biosynthesis, since the addition of cell culture eliminates the inhibitory effect of uridine metabolite A771726. With the use of radioisotope ligand shown that A771726 selectively binds to the enzyme degidroorotat dehydrogenase, which explains its properties this enzyme and inhibit proliferation of lymphocytes at the stage of G1. Simultaneously A771726 inhibits the expression of receptors for interleukin-2 and core antigen Ki-67 and PCNA, associated with the cell cycle.

Therapeutic effect of leflunomide has been shown in several experimental models of autoimmune diseases, including rheumatoid arthritis.

Pharmacokinetics

The absorption and distribution

After oral administration, absorbed 82-95% of the drug. Eating does not affect the absorption leflunamida. Leflunomide is rapidly metabolized with the formation of the active metabolite A771726. Cmax metabolite A771726 determined within 1-24 h after a single dose of the dose. In plasma A771726 rapidly binds to albumin. Untie A771726 fraction is 0.62%. Binding A771726 more variable and somewhat reduced in patients with rheumatoid arthritis or chronic renal insufficiency.

Due to the long T1 / 2 A771726 was used a loading dose of 100 mg for 3 days. Pharmacokinetic parameters A771726 have a linear dependence at doses from 5 mg to 25 mg. In these studies, the clinical effect is closely related to plasma concentration of A771726 and a daily dose of leflunomide. At a dose of 20 mg / day, mean plasma concentration of A771726 at steady-state was 35 micrograms / ml.

Metabolism

Leflunomide is rapidly metabolized in the intestinal wall and liver to one of the main (A771726) metabolite and several secondary metabolites, including 4-trifluorometilalanin. Biotransformation of leflunomide to A771726 and A771726 of the subsequent metabolism are controlled by several enzymes and occur in microsomal and other cell fractions.

Withdrawal

In plasma, urine and feces determined by the trace amounts of leflunomide. Removing A771726 slow and characterized by clearance of 31 mL / h. T1 / 2 – about 2 weeks.

Pharmacokinetics in special clinical cases

Patients on hemodialysis, elimination of the drug quickly and T1 / 2 is shorter.

Data on the pharmacokinetics in patients with liver failure are absent.

Pharmacokinetics in patients younger than 18 years has not been studied.

Elderly patients (65 years and older) pharmacokinetic data correspond approximately to the middle age group.

Indications

- As the reference drug for the treatment of active rheumatoid arthritis to reduce symptoms and delay the development of structural damage of joints.

Dosage regimen

Treatment is initiated with the appointment of a shock dose of 100 mg daily for 3 days. As a maintenance dose prescribed dose of 10 mg to 20 mg 1 time per day.

The therapeutic effect is evident after 4-6 weeks of admission and may grow within 4-6 months.

Tablets should be swallowed whole, drinking plenty of fluids.

Not require dose adjustment for patients older than 65 years.

There are currently no recommendations for dosing regime for patients with mild renal insufficiency.

Side effects

Classification of the alleged frequency of side effects: typical – 1-10%, atypical – 0.1-1%, rare – 0.01-0.1%, very rare – 0.01% or less.

Since the cardiovascular system: typical – increase blood pressure.

From the digestive system: typical – diarrhea, nausea, vomiting, anorexia, lesions of the oral mucosa (thrush, mouth ulceration), abdominal pain, increased hepatic transaminases (particularly ALT, rarely – GGT, alkaline phosphatase, bilirubin); rarely – hepatitis, jaundice, cholestasis, very rarely – liver failure, acute liver necrosis.

On the part of the musculoskeletal system: typical – abscess, atypical – the gap ligaments.

Dermatological reactions: typical – hair loss, eczema, dry skin, atypical – Stevens-Johnson syndrome, Lyell syndrome, erythema multiforme.

The part of the hemopoietic system: typical – leukopenia (white blood cells more 2000/mkl); atypical – anemia, thrombocytopenia (platelets less than 100 000/mkl); rarely – eosinophilia, leukopenia (leukocytes less 2000/mkl), pancytopenia, very rarely – agranulocytosis. The risk of hematologic disorders increases with the recent, concomitant and subsequent application of myelotoxic drugs.

Allergic reactions: typical – rash (including makulo-papular), pruritus; atypical – urticaria; very rare – anaphylactic reactions.

On the part of the exchange processes: hyperlipidemia, hypophosphatemia, reduced levels of uric acid. Laboratory data (not clinically confirmed) showed a modest increase lactate dehydrogenase, creatine phosphokinase.

Other: very rarely – the development of severe infection and sepsis may develop rhinitis, bronchitis and pneumonia. In the application of immunosuppressive drugs increases the risk of cancer and some lymphoproliferative processes.

We can not exclude the possibility of a reversible reduction of sperm concentration, total sperm count and motility.

Contraindications

- Human liver;

- Severe immunodeficiency (including AIDS);

- Pronounced disorders of bone marrow hematopoiesis or anemia, leukopenia, thrombocytopenia due to other causes (other than rheumatoid arthritis);

- Infection heavy flow;

- Moderate or severe renal insufficiency (because of the small experience of clinical observations);

- Severe hypoproteinemia (including with nephrotic syndrome);

- Pregnancy;

- Lactation (breastfeeding);

- Childhood and adolescence to 18 years;

- Hypersensitivity to the ingredients.

The drug is contraindicated in women of childbearing age who do not use adequate contraception.

Pregnancy and lactation

The drug should not be administered during pregnancy and women of childbearing age who are not using reliable contraception. You must verify the absence of pregnancy before starting treatment.

In experimental studies have found that the drug may have fetotoksicheskoe and teratogenic effect.

Patients should be informed that suspected pregnancy should seek medical advice immediately and do a pregnancy test. If the test is positive, the physician should inform the patient about the possible risk to the fetus.

Women who take leflunomide and want to become pregnant (or already in the ensuing pregnancy) procedure is recommended to launch the drug, which will rapidly reduce the concentration of leflunomide and its metabolite in blood plasma (after cessation of treatment prescribed leflunomide kolestiramin in a dose of 8 g 3 times / day within 11 days or 50 g of activated charcoal, crushed into powder, 4 times / day for 11 days).

Next, you need to determine the concentration of metabolite A771726 2 times with an interval of 14 days. From the moment when the concentration of the drug will be fixed below 20 mg / l until fertilization should take 1.5 months.

Note that without the procedure of removing the drug, reduced metabolite concentrations below 20 ug / l occurs in 2 years.

Kolestiramin and activated carbon can affect the absorption of estrogen and progesterone in such a way that reliable oral contraceptives do not guarantee the necessary contraception during launch preparation. It is recommended to use alternative methods of contraception.

Studies in animals have shown that leflunomide or its metabolites are excreted in breast milk milk. Therefore, the need to designate a lactation should resolve the issue of termination of breastfeeding.

There is currently no information confirming the link between taking the drug Arava men and fetotoksicheskim action of the drug. Experimental studies in this direction were made. However, men receiving leflunomide therapy, should be warned of the possible effect of fetotoksicheskom and the need to use adequate contraception. To minimize risk when planning pregnancy should stop taking leflunomide and use kolestiramin to 8 mg 3 times daily for 11 days or 50 grams of powdered activated charcoal 4 times daily for 11 days.

Cautions

Note that the drug Arava may be imposed only after a medical examination (including before starting treatment and during treatment should monitor blood pressure).

Before treatment drug Arava should be mindful of possible increase in the number of side effects in patients previously treated with other basic tools for the treatment of rheumatoid arthritis, which have hepato-and gematotoksicheskim action.

The active metabolite of leflunomide A771726 characterized by long T1 / 2. Therefore, side effects can occur even after cessation of therapy. If you have any similar cases of toxicity or when moving to another base receiving the drug after treatment with leflunomide should be the procedure of removing the drug (after the cessation of leflunomide treatment prescribed kolestiramin in a dose of 8 g 3 times daily for 11 days or 50 g of activated carbon, crushed to powder, 4 times / day for 11 days).

Note that during the development of severe dermatologic adverse reactions, severe infections receiving the drug Arava should stop and immediately initiate the removal of the drug.

Need to monitor patients with tuberculin reactivity due to the risk of activating tuberculosis.

Given the long-term elimination of Arava is not recommended to vaccinate live vaccines against a background of leflunomide treatment.

Overdose

No data on overdose of leflunomide. Admission leflunomide 100 mg daily for 14 days was observed in 10 healthy volunteers. Two of them were removed after a week because of the increased level of transaminases in the blood plasma.

In case of overdose or toxicity is recommended to use kolestiramina or powdered activated carbon. Kolestiramin, take 3 healthy volunteers administered orally to 8 mg 3 times / day during the day, reduced levels of A771726 in plasma by approximately 40% after 24 h and 49-65% after 48 h.

Shown that introduction of activated charcoal orally or via oral gavage (50 mg every 6 hours during the day) reduced the concentration of the active metabolite A771726 in plasma by 37% after 24 h and 48% after 48 h.

Perhaps repetition procedures are preparation for clinical indications.

Drug Interactions

Increased adverse reactions may occur in the case of recent or concomitant use of hepatotoxic drugs or hematotoxicity or when receiving these drugs after starting leflunomide treatment procedure without removing the drug.

Not observed pharmacokinetic interaction between leflunomide (10-20 mg / day) and methotrexate (10-25 mg / week).

Unknown clinically significant interactions with concomitant use of leflunomide and triphasic oral contraceptives, NSAIDs, cimetidine, rifampicin.

Studies in vitro showed that the metabolite of leflunomide A771726 inhibits the activity of cytochrome P450 2C9. Therefore, caution should be prescribed the drug Arava with drugs metabolized by this enzyme system (phenytoin, warfarin, tolbutamide).


Conditions and terms of storage

The product should be stored at temperatures not above 25 ° C. Shelf life – 3 years.

Conditions of supply of pharmacies

The drug is released with a prescription.

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Cozaar

Latin name
Cozaar ®
ATC:
>> C09CA01 Losartan
Pharmacological Group
>> Receptor antagonists of angiotensin II (AT1-subtype)
Nosological classification (ICD-10)
>> I10-I15 Diseases characterized by high blood pressure
>> I50 Heart failure
The composition and the form
1 tablet contains losartan potassium 12.5 or 50 mg in the contour of cellular packing 21 or 14 pieces., In box 2 and 1 pack respectively.
Pharmacological action
Mode of action – hypotensive. Blocks angiotensin II (type AT1) reduces OPSS, reduces afterload, reduces systemic blood pressure and the pressure in the lesser circulation.
Pharmacokinetics
Well absorbed. Be distributed relatively evenly. Metabolized to form the active derivative.
Pharmacodynamics
Maximum antihypertensive effect is achieved within 3-6 weeks of treatment.
Indications
Arterial hypertension, heart failure (including when treatment with ACE inhibitors is no longer appropriate for the patient.
Contraindications
Hypersensitivity, children’s age.
Application of pregnancy and breastfeeding
When the reception immediately terminate pregnancy (may cause developmental defects or fetal death, especially in the II-III trimester). Nursing mothers should stop breastfeeding.
Side effects
Dizziness, hypotension (dose-related), hyperkalemia (1.5% of patients).
Interaction
Compatible with other antihypertensive agents. Against the background of diuretics (high doses) increases the risk of excessive hypotension in patients with dehydration.
Overdose
The most likely manifestation – hypotension and tachycardia (possible vagal bradycardia). Treatment of symptomatic – no Kozaar nor its active metabolite are not displayed hemodialysis.
Dosing and Administration
Inside, regardless of the meal, once. Usually – 50 mg / day. In some cases, to achieve greater effect, increase the dose to 100 mg. Patients with dehydration may make an initial dose of 25 mg / day. For patients with heart failure the initial dose may reach 12.5 mg 1 time per day.
Precautions
Patients with a history of liver disease should be prescribed lower doses (plasma concentration significantly increased for violations of its functions, especially with cirrhosis).
Expiration
3 years
Storage
List B.: In the dark place at a temperature not above 25 ° C.
Date update
2001-07-31

Latin name

Cozaar ®

ATC:

>> C09CA01 Losartan

Pharmacological Group

>> Receptor antagonists of angiotensin II (AT1-subtype)

Nosological classification (ICD-10)

>> I10-I15 Diseases characterized by high blood pressure

>> I50 Heart failure

The composition and the form

1 tablet contains losartan potassium 12.5 or 50 mg in the contour of cellular packing 21 or 14 pieces., In box 2 and 1 pack respectively.

Pharmacological action

Mode of action – hypotensive. Blocks angiotensin II (type AT1) reduces OPSS, reduces afterload, reduces systemic blood pressure and the pressure in the lesser circulation.

Pharmacokinetics

Well absorbed. Be distributed relatively evenly. Metabolized to form the active derivative.

Pharmacodynamics

Maximum antihypertensive effect is achieved within 3-6 weeks of treatment.

Indications

Arterial hypertension, heart failure (including when treatment with ACE inhibitors is no longer appropriate for the patient.

Contraindications

Hypersensitivity, children’s age.

Application of pregnancy and breastfeeding

When the reception immediately terminate pregnancy (may cause developmental defects or fetal death, especially in the II-III trimester). Nursing mothers should stop breastfeeding.

Side effects

Dizziness, hypotension (dose-related), hyperkalemia (1.5% of patients).

Interaction

Compatible with other antihypertensive agents. Against the background of diuretics (high doses) increases the risk of excessive hypotension in patients with dehydration.

Overdose

The most likely manifestation – hypotension and tachycardia (possible vagal bradycardia). Treatment of symptomatic – no Kozaar nor its active metabolite are not displayed hemodialysis.

Dosing and Administration

Inside, regardless of the meal, once. Usually – 50 mg / day. In some cases, to achieve greater effect, increase the dose to 100 mg. Patients with dehydration may make an initial dose of 25 mg / day. For patients with heart failure the initial dose may reach 12.5 mg 1 time per day.

Precautions

Patients with a history of liver disease should be prescribed lower doses (plasma concentration significantly increased for violations of its functions, especially with cirrhosis).

Expiration

3 years

Storage

List B.: In the dark place at a temperature not above 25 ° C.

Date update

2001-07-31

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Coumadin

Coumadin – Warfarin
Coumadin should be taken strictly in accordance with a medical prescription.
If you are over 60 years, then as a rule, you should take a lower dose than is usually assigned to reduce the risk of bleeding
Taken once a day, preferably at the same time
After three months of the reception, your doctor should reassess the need to continue taking Coumadin.
In the case of misuse, Coumadin can cause serious side effects: haemorrhage, bleeding, bruises, red spots on the body, irritation and skin damage.
Precautions – protection against shock, falls, cuts – even insect bites can lead to hemorrhage.
Fractures, traumatic injuries, blows to the stomach – can lead to massive bleeding, blood loss and death, and therefore should take action and nemedlennopoluchit immediate medical attention!
During the reception Coumadin, your doctor should monitor your condition through regular blood PT / INR (Pi.Ti.) and change in dosage if necessary, to ensure maximum efficiency of treatment.
Coumadin interacts with virtually all drugs. Its anticoagulant effect is very difficult to control, if the period of his admission begins or ceases to use or change the dose of another drug. Another drug can amplify or weaken the effect of Coumadin.
During the reception Coumadin should not take any other medicines, including OTC drugs (eg aspirin, cold remedies, antacid, laxative), or change the dose, which you are currently taking, without first talking to your doctor.
Note the interaction with Coumadin Paracetamol (Akamol-Deksamol) – the risk of bleeding increases tenfold!
Talk to your doctor, how to behave in case of need anesthesia.
Analysis – PT / INR as balancing performance and prescribed by the doctor once every 3 months: hemoglobin, platelet count, liver function tests, albumin, liver enzymes, kidney parameters, bleeding time, tests of functional activity of platelets
Take Coumadin dose should agree with the doctor, depending on the result of the analysis of PT / INR.
Do not take the responsibility for the appointment dose lekarstva.Tolko doctor can and knows how to take and will give you a diagram.
It is important to draw attention to the fact that interaction coumadin vegetables green.
Since Coumadin interacts with vitamin K, while taking Coumadin prohibited use food white cabbage (even fermented), red, color, Brussels sprouts, broccoli, cilantro, parsley, celery, fennel (green), lettuce, green onions, green peas, green beans, avocado

Coumadin – Warfarin

Coumadin should be taken strictly in accordance with a medical prescription.


If you are over 60 years, then as a rule, you should take a lower dose than is usually assigned to reduce the risk of bleeding


Taken once a day, preferably at the same time


After three months of the reception, your doctor should reassess the need to continue taking Coumadin.


In the case of misuse, Coumadin can cause serious side effects: haemorrhage, bleeding, bruises, red spots on the body, irritation and skin damage.


Precautions – protection against shock, falls, cuts – even insect bites can lead to hemorrhage.

Fractures, traumatic injuries, blows to the stomach – can lead to massive bleeding, blood loss and death, and therefore should take action and nemedlennopoluchit immediate medical attention!


During the reception Coumadin, your doctor should monitor your condition through regular blood PT / INR (Pi.Ti.) and change in dosage if necessary, to ensure maximum efficiency of treatment.


Coumadin interacts with virtually all drugs. Its anticoagulant effect is very difficult to control, if the period of his admission begins or ceases to use or change the dose of another drug. Another drug can amplify or weaken the effect of Coumadin.


During the reception Coumadin should not take any other medicines, including OTC drugs (eg aspirin, cold remedies, antacid, laxative), or change the dose, which you are currently taking, without first talking to your doctor.

Note the interaction with Coumadin Paracetamol (Akamol-Deksamol) – the risk of bleeding increases tenfold!


Talk to your doctor, how to behave in case of need anesthesia.


Analysis – PT / INR as balancing performance and prescribed by the doctor once every 3 months: hemoglobin, platelet count, liver function tests, albumin, liver enzymes, kidney parameters, bleeding time, tests of functional activity of platelets


Take Coumadin dose should agree with the doctor, depending on the result of the analysis of PT / INR.

Do not take the responsibility for the appointment dose lekarstva.Tolko doctor can and knows how to take and will give you a diagram.


It is important to draw attention to the fact that interaction coumadin vegetables green.


Since Coumadin interacts with vitamin K, while taking Coumadin prohibited use food white cabbage (even fermented), red, color, Brussels sprouts, broccoli, cilantro, parsley, celery, fennel (green), lettuce, green onions, green peas, green beans, avocado.

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