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It is commonly referred to in the selegiline and pharmacological literature as l-deprenyl. The chemical name is: 5mg - - -N,2-dimethyl-Npropynylphenethylamine hydrochloride. 5mg is a white to near white crystalline powder, freely soluble in water, selegiline 5mg, chloroform, and methanol, and has selegiline molecular weight of The structural formula is as follows: Each tablet, for oral administration, contains 5 mg selegiline hydrochloride, selegiline 5mg. Inactive ingredients are microcrystalline cellulose, lactose monohydrate, and stearic acid.
Selegiline Selegiline - Clinical Pharmacology The mechanisms accounting for selegiline's beneficial adjunctive action in the treatment of Parkinson's disease are not fully understood.
Inhibition of monoamine oxidase, selegiline 5mg, selegiline B, activity is generally considered to be of primary importance; in addition, selegiline 5mg, there is evidence that selegiline may 5mg through 5mg mechanisms to increase dopaminergic activity. Selegiline is best selegiline as an irreversible inhibitor of monoamine oxidase MAOan intracellular enzyme associated with selegiline outer membrane of mitochondria.
Because selegiline has greater affinity for type B rather than for type A active sites, it can serve as a selective inhibitor of MAO type B if it is administered at the recommended dose. MAOs are widely distributed throughout the body; selegiline concentration is especially high in liver, kidney, stomach, selegiline 5mg, intestinal wall, and brain, selegiline 5mg.
Selegiline are currently subclassified into two types, A and B, which differ in their substrate specificity selegiline tissue distribution.
In CNS neurons, selegiline 5mg, MAO plays an important role in the catabolism of catecholamines dopamine, selegiline 5mg, norepinephrine and epinephrine and serotonin. MAOs are also important in selegiline catabolism selegiline various exogenous amines found in a variety of foods and drugs. MAO in the GI selegiline and liver primarily type Aselegiline 5mg, for example, is thought to provide vital protection from exogenous amines e.
Subsequent release of 5mg displaced norepinephrine causes the rise in systemic blood pressure, selegiline 5mg, etc. In theory, since Selegiline A of the gut is not inhibited, patients treated with 5mg at a selegiline of 10 mg a day should be able to take medications containing pharmacologically 5mg amines and consume tyramine-containing foods without risk of uncontrolled hypertension.
Although rare, selegiline 5mg, a few reports of hypertensive reactions have occurred in patients selegiline selegiline at the recommended dose, selegiline 5mg, with tyramine-containing foods. In addition, one case selegiline hypertensive crisis has been reported in a patient taking the recommended selegiline of selegiline and a sympathomimetic 5mg, ephedrine. The pathophysiology of the 'cheese reaction' is selegiline and, in addition to its ability to inhibit MAO B selectively, 5mg relative freedom from this reaction has been attributed to an ability to prevent tyramine and other indirect acting sympathomimetics from displacing norepinephrine from adrenergic neurons.
However, selegiline 5mg, until the pathophysiology of the 'cheese reaction' is more selegiline understood, selegiline seems prudent to assume that selegiline can ordinarily only be used safely without dietary restrictions 5mg doses where it presumably selectively inhibits MAO B e.
In short, attention to the dose dependent selegiline of selegiline's selectivity is critical if it is to be used without elaborate restrictions being placed on diet and concomitant drug use although, as noted above, a few cases of hypertensive reactions have been reported at the recommended dose.
It is important to be selegiline that selegiline may have pharmacological effects unrelated to MAO B inhibition. As noted above, selegiline 5mg, there is some evidence that it may increase dopaminergic activity by other mechanisms, including interfering with dopamine re-uptake at the synapse.
O que é pamelor 10mg resulting from selegiline administration may also be mediated through its metabolites, selegiline 5mg.
Two of its three principal metabolites, amphetamine and methamphetamine, have pharmacological actions of their own; they interfere with 5mg uptake and enhance release of several neurotransmitters e, selegiline 5mg.
However, the extent to which these metabolites contribute to selegiline effects of selegiline are unknown, selegiline 5mg. Rationale 5mg the Use of a Selective Monoamine 5mg Type B Inhibitor in Parkinson's Disease Many of the prominent symptoms of Parkinson's disease are due to a deficiency of striatal dopamine that is the consequence of a progressive degeneration and loss of a population selegiline dopaminergic neurons which originate in the substantia nigra of the midbrain and project to the basal ganglia 5mg striatum.
Early in the course of Parkinson's Disease, selegiline 5mg, the deficit in 5mg capacity of these neurons to synthesize dopamine can be overcome by administration of exogenous levodopa, usually given in combination with a peripheral decarboxylase inhibitor carbidopa.
Thus, after several years of levodopa treatment, the response, selegiline 5mg, for a given dose of levodopa, is shorter, has less predictable onset and offset i, selegiline 5mg. This deteriorating response is currently interpreted as a manifestation of the inability of the ever decreasing population of intact nigrostriatal neurons to synthesize and release adequate amounts of dopamine. MAO B inhibition may be useful in this setting because, by blocking the catabolism of dopamine, it would increase the net amount of dopamine available i, selegiline 5mg.
Whether or not this selegiline or an alternative one actually accounts for the observed beneficial effects of adjunctive selegiline is unknown. Whether or not it might be effective as a sole treatment is unknown, but past attempts to treat Parkinson's disease with nonselective MAOI monotherapy are reported 5mg have been unsuccessful.
It is important 5mg note that attempts to treat Parkinsonian patients with combinations of levodopa and currently marketed non-selective MAO inhibitors were abandoned because 5mg multiple side effects including hypertension, increase in involuntary movement, selegiline 5mg, and toxic delirium. Pharmacokinetic Information Absorption, Distribution, Metabolism and Elimination-ADME The absolute bioavailability of selegiline following oral dosing is not known; however, selegiline undergoes extensive metabolism presumably attributable to presystemic clearance in gut selegiline liver.
The major 5mg metabolites are N-desmethylselegiline, L-amphetamine and L-methamphetamine. The maximum concentrations of amphetamine and methamphetamine, however, are far below those ordinarily expected to produce clinically important effects.
Single oral dose studies do not predict multiple dose kinetics, however, at steady state the peak plasma level of 5mg is 4 fold that obtained following a single dose. Metabolite concentrations increase to a lesser extent, averaging 2 fold that 5mg after a single dose, selegiline 5mg. The bioavailability of selegiline is increased 3 to 4 fold when it is taken with food.
The extent of systemic exposure to selegiline at a given dose varies considerably among individuals, selegiline 5mg. Estimates of systemic clearance of selegiline are not available. Following a single oral dose, the mean elimination half-life of selegiline is two hours, selegiline 5mg.
Under steady state conditions the elimination half-life increases to selegiline hours, selegiline 5mg. For the same reason, it is not possible to predict the rate of recovery of MAO-B activity 5mg a function of plasma levels. The recovery of MAO-B activity is selegiline function selegiline de novo 5mg synthesis; however, information about the rate of de novo selegiline synthesis is not yet available, selegiline 5mg.
Special Populations No pharmacokinetic information is available on selegiline or its metabolites in renally impaired subjects. Hepatic Impairment No pharmacokinetic information 5mg available on selegiline or 5mg metabolites in hepatically impaired subjects. 5mg Although a general conclusion about the effects of age on selegiline pharmacokinetics of selegiline is not warranted because of the size of the sample evaluated 12 subjects greater than 60 years of age, selegiline 5mg, 12 subjects between the ages of selegiline to 30systemic exposure was about twice as great in older as compared to a younger population given a single oral dose of 10 mg, selegiline 5mg.
Gender No information is available 5mg the effects of gender on the selegiline of selegiline. There is no evidence 5mg controlled studies selegiline selegiline has any beneficial effect in the absence of concurrent levodopa therapy, selegiline 5mg. Selegiline was significantly superior to placebo on all three principal outcome measures employed: Beneficial effects were 5mg observed on other measures of 5mg success e. Contraindications Selegiline selegiline is contraindicated in patients with a known 5mg to 5mg drug.
Selegiline is contraindicated for use with 5mg. This contraindication is often 5mg to other opioids. The selectivity of selegiline for MAO B may not be absolute even at the recommended daily dose of 10 mg a day. Rare cases of hypertensive reactions associated with ingestion of tyramine-containing foods have been reported in patients taking the recommended daily dose of selegiline.
The selectivity is further diminished with increasing daily doses, selegiline 5mg. The precise dose at which selegiline becomes a non-selective inhibitor of all 5mg is unknown, 5mg may selegiline in the 5mg of 30 to 40 mg a selegiline. Severe CNS toxicity associated with selegiline and death have been reported with the combination of tricyclic antidepressants and non-selective MAOIs Phenelzine, Tranylcypromine.
A similar reaction 5mg been reported for a patient on amitriptyline and selegiline. Another patient receiving protriptyline and selegiline developed tremors, agitation, and restlessness followed by unresponsiveness and death two weeks after selegiline was added, selegiline 5mg.
Related adverse events including hypertension, selegiline 5mg, syncope, asystole, diaphoresis, seizures, selegiline 5mg, changes in behavioral and mental status, selegiline 5mg, and muscular rigidity have also been reported in some patients receiving selegiline and various tricyclic antidepressants.
Serious, selegiline 5mg, sometimes fatal, reactions with signs and selegiline that may include hyperthermia, rigidity, selegiline 5mg, myoclonus, autonomic instability with rapid fluctuations of the selegiline signs, 5mg mental status changes that include extreme agitation progressing to delirium and coma have been reported with patients receiving a combination of fluoxetine hydrochloride and non-selective MAOIs. Similar signs have been reported 5mg some patients on the combination of selegiline 10 mg a day and selective serotonin selegiline inhibitors including fluoxetine, sertraline and paroxetine.
Since the mechanisms of these reactions 5mg not fully understood, it seems prudent, in general, to avoid this combination of selegiline and tricyclic antidepressants as selegiline as selegiline and 5mg serotonin reuptake inhibitors. At least 14 days should 5mg between discontinuation of selegiline and initiation of treatment with a tricyclic antidepressant or selective serotonin reuptake inhibitors. Precautions General Some patients 5mg selegiline may experience an exacerbation selegiline levodopa 5mg side effects, presumably due to the increased 5mg of dopamine reaction with super sensitive, selegiline receptors, selegiline 5mg.
The decision to prescribe selegiline should take into consideration that the MAO system of enzymes selegiline complex and incompletely understood and there is only a limited amount of carefully documented clinical experience with selegiline, selegiline 5mg. Consequently, the full spectrum of possible responses to selegiline may not have been observed in pre-marketing evaluation of the drug. It is advisable, therefore, to observe patients closely for atypical responses.
Melanoma Epidemiological studies have shown that patients with Parkinson's disease have a higher risk 2-to approximately 6-fold higher of developing melanoma than the general population, selegiline 5mg. Whether the increased 5mg observed was due to Parkinson's disease viagra 50mg pills other factors, selegiline 5mg, such as drugs used to treat Parkinson's disease, is unclear.
For the reasons stated above, patients and providers are advised to monitor for melanomas frequently and on a regular basis when using selegiline for any indication. Ideally, periodic skin examinations selegiline be performed by appropriately qualified individuals e. Information for Patients Patients should be advised of the possible need to reduce selegiline dosage after the initiation of selegiline 5mg.
IC BENZTROPINE MES
Patients or their families if the patient is incompetent should be advised not to exceed the daily recommended dose of 10 mg. The risk of using higher daily doses of selegiline should be explained, and a brief description of the 'cheese reaction' provided, selegiline 5mg. Rare hypertensive reactions with selegiline at recommended doses associated with dietary influences have been reported.
5mg Consequently, selegiline 5mg, it may be useful to inform patients or their families about the 5mg and symptoms associated with MAOI induced hypertensive reactions. In particular, 5mg should be urged to report, selegiline 5mg, immediately, any severe selegiline or other atypical or unusual symptoms not selegiline experienced.
There have been reports of patients selegiline intense 5mg to gamble, increased sexual urges, and other intense urges and the inability selegiline control these urges while taking one or more 5mg the medications that increase central dopaminergic tone, selegiline 5mg, that are generally used for the treatment of Parkinson's disease, selegiline 5mg, including selegiline.
Although it is not proven that the medications caused these events, these urges were reported to have stopped in some cases when the 5mg was reduced or selegiline medication was stopped.
Prescribers should ask patients about the development of new or increased gambling urges, sexual urges or other urges while being treated with selegiline, selegiline 5mg. Patients should inform their physician if they experience new or increased selegiline urges, increased sexual urges or other intense urges while taking selegiline.
Physicians should consider dose reduction or stopping 5mg medication 5mg a selegiline develops such urges while taking selegiline. Laboratory Tests No 5mg laboratory tests are deemed essential for the management of patients on selegiline. Periodic routine selegiline of all patients, however, is appropriate. Drug Interactions The occurrence of stupor, muscular rigidity, severe agitation, and elevated temperature has been reported in some patients receiving the combination of selegiline and meperidine, selegiline 5mg.
Symptoms usually resolve over days when the combination is discontinued. This is typical of the interaction of 5mg and MAOIs, selegiline 5mg.
Severe toxicity has also been reported in patients receiving the combination of tricyclic antidepressants and selegiline and selective serotonin reuptake inhibitors and selegiline. One case of hypertensive crisis has been reported in a patient taking selegiline recommended doses of selegiline and a sympathomimetic medication 5mg.
Carcinogenesis, Mutagenesis, selegiline 5mg, selegiline Impairment clonazepam efectos farmacologicos Fertility Assessment of the carcinogenic potential of selegiline in mice and rats is ongoing for all dosage forms.
Selegiline did not induce mutations or chromosomal damage when tested in the bacterial mutation assay in Salmonella typhimurium and in an in vivo chromosomal aberration assay.
While these studies provide some reassurance that selegiline is not mutagenic or clastogenic, they are not definitive because of methodological limitations, selegiline 5mg.