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Ritalin stimulates the mind and body in adults and can calm children down.

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The powders and crystals tend to be white or off-white in colour, while the pellets and tablets can be different colours.

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Learn More. Side effects are usually mild and are generally well tolerated by patients. Along with increases in prescribing frequency, the potential for abuse has increased. Intranasal abuse produces effects rapidly that are similar to the effects of cocaine in both onset and type. The clinical picture of stimulant abuse produces a wide array of psychiatric symptoms. There is little in the literature to differentiate methylphenidate from other stimulants when they are abused. The need for education of all involved with the use of methylphenidate is discussed to help prevent an increasing pattern of methylphenidate abuse.

It has also been used to treat other disorders such as depression, narcolepsy, brain injury, cancer, pain, and cognitive disorders and to treat patients with human immunodeficiency virus infection. However, the entire therapeutic profile starts to change when it is abused.

As ADHD is more accurately diagnosed and treated appropriately with stimulant medication, there will be a continued increase in the amount of methylphenidate prescribed and dispensed.

Abuse often entails the use of large doses, which may be taken intranasally or intravenously. This article will review the pharmacology of methylphenidate and look at its psychiatric side effects when abused. Patterns of abuse, including intranasal use, will also be discussed to help the primary care practitioner become more aware of some of the potential problems when monitoring and supervising the use of methylphenidate. Methylphenidate, synthesized in 13 and patented inwas first marketed by Ciba-Geigy Pharmaceutical Company as Ritalin.

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It was initially first used in for a of indications. Methylphenidate has become the drug of first choice prescribed by many physicians for the initial treatment of ADHD. Methylphenidate is classified as a CNS stimulant. Its proposed mechanism of action is the release and increase of CNS dopamine. This increase provides the needed stimulation and proposed activation of the motor inhibitory system in the orbital-frontal-limbic axis.

Therefore, this medication assists children with ADHD by helping them focus their attention when necessary.

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The exact mechanism of action of methylphenidate is dissimilar to that of the amphetamines and cocaine, yet the net effect is an increase in synaptic dopamine. Radiographic studies with 11 C -labeled methylphenidate and cocaine have found the binding of both drugs to be localized in the same brain region, the striatum.

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Upon oral administration, methylphenidate is rapidly and completely absorbed from the gastrointestinal tract. Peak concentrations occur 1 to 2 hours 25 after dose administration. The pharmacokinetic half-life of methylphenidate is approximately 2 hours 25 and ranges from 2 to 7 hours. When methylphenidate and cocaine are administered intravenously, their pharmacokinetics are quite similar. Volkow and colleagues 22 found that the percentage of each drug taken up by the brain and their rates of uptake were parallel.

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When methylphenidate is abused intranasally, the effects are usually similar to intranasal use of amphetamines and crack cocaine. The potential for abuse is emphasized throughout the literature and should serve as a warning to clinicians. However, this warning is often overshadowed by the many patients who have a positive therapeutic response to oral methylphenidate and do not abuse it. When used intranasally, methylphenidate has receptor effects similar to those of cocaine.

Thus, the clinical picture of abuse is often quite similar to that of cocaine. Methylphenidate can be transformed from a therapeutic agent to an abused and addictive substance when this drug is taken in excessive amounts and used through intranasal and intravenous routes. Availability is often an integral part of a drug's abuse potential, and the availability of methylphenidate is certainly increasing. According to the Drug Enforcement Agency DEAthe production of methylphenidate in the United States has increased from kilograms in to 10, kilograms in with a 6-fold increase in production from to Ignorance of this potential for abuse starts early as described in a survey of school-aged children who were asked about the drug Ritalin.

How fast a drug works often predicts its abuse potential and reinforcement liability. As mentioned ly, when administered intravenously, these drugs are indistinguishable and have a parallel rate of uptake into the brain cocaine: 4—6 minutes, methylphenidate: 4—8 minutes. In the early s, the abuse potential of methylphenidate was questioned in a case report of a patient who was taking tablets of methylphenidate daily.

Intravenous abuse of methylphenidate associated with psychosis was noted in 43 followed by several reports of intravenous abuse in the early s. Intranasal abuse has not been scientifically assessed, but the occurrence and effects have been demonstrated through case reports in the literature.

The first report of intranasal abuse of methylphenidate 33 appeared in A DEA document reports 2 cases of health professionals abusing intranasal methylphenidate. An additional case of abuse by a year-old boy with ADHD 50 was reported in The boy had a 2-week history of methylphenidate abuse that started with feelings of euphoria and ended in paranoia, depression, and suicidal ideation.

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A recent case in the literature 51 describes the death of a year-old teen following abuse of intranasal methylphenidate. The teenager lost consciousness, fell, hit his head, and then went into cardiopulmonary arrest. Toxicologic analyses confirmed the presence of methylphenidate and alcohol. Acute toxicity due to methylphenidate overdose in symptoms similar to those of acute amphetamine intoxication. Reports of psychiatric symptoms that have occurred include euphoria, delirium, confusion, toxic psychosis, and hallucinations.

There are limited data in the literature regarding the psychiatric side effects of methylphenidate when it is abused. Most of the data are found in case reports and are often reported as similar to the psychiatric side effects of amphetamines or cocaine.

The clinical picture of the effects of high-dose methylphenidate resembles that of amphetamine intoxication and psychosis. The presentation of this psychiatric picture is often quite dramatic, but is transient and has been seen with all major stimulants, including methylphenidate. Psychiatric symptoms of extreme anger with threats of aggressive behavior may occur in methylphenidate abuse. When high doses are taken, delirium, aggressiveness, panic states, and hallucinations have been observed. Psychological and behavioral symptoms of amphetamine use are listed in Table 1.

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When abused, methylphenidate produces toxicity similar to other CNS stimulant overdoses. The clinical picture of stimulant intoxication produces a wide array of symptoms including schizophrenic symptoms, manic-like states, psychoses, depressions especially during withdrawaland various types of anxiety conditions including panic states. Psychiatric symptoms of stimulant overdose may include hallucinations, delusions, paranoia, confusion, disorientation, and loose association of ideas.

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These psychiatric and physical side effects resolve over a period of hours to weeks. Some abusers may experience increasing effects after multiple doses similar to sensitizationwhile others experience severe effects from small doses reverse tolerance. In addition, homicide related to amphetamine intoxication has been reported.

This suspiciousness combined with impaired judgment and insight can be a catalyst for violence and murder. To summarize, the psychiatric side effects of methylphenidate are quite similar to those of cocaine and amphetamines, giving more support to the idea that almost all CNS stimulants will produce a similar clinical picture. A person using cocaine can experience nervousness, 57, 58 restlessness, 58 agitation, 57 suspiciousness, 60 paranoia, 61—63 hallucinations and delusions, 61, 63 impaired cognitive functions, 64 delirium, 65 violence, 57, 58, 62, 65, 66 suicide, 67 and homicide.

The potential for methylphenidate abuse has been addressed primarily through regulatory measures. These include regulating the amount of methylphenidate able to be filled at pharmacies during a specified time period and adding a higher level of surveillance by asing it to schedule II status. Other measures to reduce abuse include encouraging tablet counts by parents and considering changing to stimulants that do not require a dose in the middle of the day, thereby decreasing handling by children in schools. Given the potential for abuse, methylphenidate merits being maintained as a schedule II drug despite parental requests to deregulate it.

Prevention of methylphenidate abuse needs to be a shared responsibility between the practitioner, the parents, and the patient. All participants in therapy need to be educated about the abuse potential of methylphenidate. The history and emerging patterns of abuse as outlined in Table 2 will help sensitize practitioners and patients to the risk of abuse. Practitioners need to address such issues as the consequences of excessive use or intranasal use as well as other abuse patterns.

How does ritalin work in the body?

The use of methylphenidate by anyone other than the patient to whom it was prescribed needs to be addressed and caution maintained throughout therapy. The extreme consequences of abuse and addiction, resulting in legal repercussions, psychiatric symptoms and disorders, as well as death and homicide, need to be discussed seriously.

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Education must originate with the prescriber. Increasing practitioner awareness of the pharmacologic, psychological, and physiologic similarities with cocaine is essential to avoid potential abuse.

The medical and treatment communities need to be aware of these potential problems, and primary care practitioners need to be aware of the problems associated with methylphenidate abuse, recognize the abuse patterns, and take a strong position in educating all those concerned with methylphenidate use.

Drug names: amphetamine Adderalldextroamphetamine Dexedrine and othersmethamphetamine Desoxynmethylphenidate Ritalin and others. National Center for Biotechnology InformationU. Alexander MortonPharm. StocktonPharm.

Why does the means of administration matter?

Author information Article notes Copyright and information Disclaimer. Reprint requests to: W. Alexander Morton, Pharm. BoxCharleston, SC e-mail: ude. Received Aug 9; Accepted Sep This article has been cited by other articles in PMC. Intranasal Abuse Intranasal abuse has not been scientifically assessed, but the occurrence and effects have been demonstrated through case reports in the literature.

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