New and re-emerging Abused Drugs

September 27, 2014

New and re-emerging Abused Drugs

Prescription-Drug-Abuse The greatest challenge for physicians today is to be up to par with the new and remerging drugs of abuse. The problem is the law enforcers have declared certain drugs that were perceived to have medicinal qualities into illegal drugs. Most of these drugs are those used in cooling pain. Having these drugs classified as illegal has led to many street doctors to adopt ways through which they can continue using such drugs without being at loggerheads with the law enforcers and that has led to mixing certain substances with these drugs in a bid to conceal what the real contents of the drugs are. They have also branded this drugs with strange names all in a in a bid to hide them from the law enforcers. The packages of these drugs are written as ‘not for human consumption’ among other strange names that has been given to these new and re-emerging drugs of abuse to enable them trade safe. Emerging drugs of abuse are forever changing and involve manipulation of basic chemical structures to avoid legal ramifications. The structural changes are important to those dealing in these drugs as they help them evade forensic chemical tests hurdles. The names given to these drugs may not even have a relation to their contents and so not as important as understanding the classes of these drugs. Most of the synthetic new drugs of abuse result in psychoactive and sympathomimetic effects.

For emphasis this needs to be repeated many of these drugs are marketed as “legal highs despite being labeled “not for human consumption” to avoid regulation. The availability of these substances over the Internet and in “head shops” has led to a multitude of emergency department visits with severe complications including deaths worldwide. Today there are still new drugs of abuse that are not yet known by physicians. The drugs are not easy to tame since even the slightest alterations of the basic chemical structure of substances create an entirely new drug no longer regulated by current laws and an ever-changing landscape of clinical effects. The purity of each substance with exact pharmacokinetic and toxicity profiles is largely unknown hence very dangerous to the users. Some of these drugs that are being abused greatly today hence not very easy to tame are piperazines.

Piperazines

Piperazines have often been referred to as failed pharmaceuticals. This is because some had been evaluated as potential therapeutic agents by pharmaceutical companies but never brought to the market .One piperazine that has been commonly used as NPS is 1-benzylpiperazine (BZP) though other piperazine derivatives have also been reported to be useful in medicine. These include among others 1-(3-chlorophenyl) piperazine (mCPP), 1-(3-trifluoromethylphenyl) piperazines (TFMPP), 1-benzyl-4-methylpiperazine (MBZP), 1-(4-fluorophenyl) piperazines (pFPP) and 1-cyclohexyl-4-(1,2-diphenylethyl) piperazine (MT-45).

BZP itself was initially developed as a potential antidepressant drug, but was found to have similar properties to amphetamine and therefore liable to abuse. In the 1980s, it was used in Hungary to manufacture piberaline, a substance marketed as an antidepressant. This substance was later withdrawn since it was thought liable to abuse as well. In the late 1990s, BZP emerged in New Zealand as a ‘legal alternative’ for MDMA and methamphetamine. In Europe, its use was first reported in Sweden in 1999, but it only became widespread as a NPS from 2004 onwards until controls over the substance were introduced in 2008, in the European Union. mCPP was developed during the late 1970s and is used as an intermediate in the manufacture of several antidepressants, e.g. trazodone and nefazodone. TFMPP is almost always seen in combination with BZP to produce the entactogenic effects of MDMA.

Neither BZP nor any other piperazines are under international control, although several (BZP, TFMPP, mCPP, MDBP) were pre-reviewed by the WHO Expert Committee on Drug Dependence in 2012. Several countries have introduced national control measures over piperazines. The control measures are however still challenged as those dealing in these drugs are adopting ways to beat the authorities in this trade. Piperazines are frequently sold as ‘ecstasy’. Some of the generic names for these substances include; pep pills, social tonics or simply as party pills.

These drugs are mostly used recreationally and two groups of these drugs feature here and these are benzylpiperazines and phenylpiperazines. Most of the pills sold as ecstasy and amphetamines have been found to contain components of Piperazines or its substitutes. They can also come as mixtures of more than one piperazine (such as BZP/TFMPP) or in combination with other drugs of abuse. Today Piperazines are some of the most common active substances found in Internet purchased drugs and they are majorly abused by young people.

Can adversely affect the users

Piperazines have been found to act as stimulants as a result of dopaminergic, noradrenergic, and predominantly serotoninergic effects produced in the brain. The majority of pharmacological studies of piperazines has focused on BZP and have indicated that it produces toxic effects similar to amphetamine and other sympathomimetics. According to animal studies, its effects are less potent than amphetamine, methamphetamine and MDMA. TFMPP, used in conjunction with BZP, has been reported to produce some of the effects of MDMA, but with a lower potency, while mCPP has been indicated to produce similar stimulant and hallucinogenic effects as MDMA.

In New Zealand, toxic seizures and respiratory acidosis after the use of BZP alone or in conjunction with other drugs were reported from three patients. Another study of 61 patients reported toxic effects of BZP, with two cases presenting life-threatening toxicity. Hyperthermia, rhabdomyolysis and renal failure associated with BZP ingestion have also been reported. In the United Kingdom, self-terminating grand mal seizures after the use of BZP have also been reported. All these findings prove how fatal the use of these drugs is and so should be avoided at all costs.

Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.

New and re-emerging Abused Drugs

Ketamine Intoxication Abuse Could Lead To Dependence

September 26, 2014

Ketamine Intoxication Abuse and Dependence

Ketamine Intoxication Any drug when taken for non-medical purposes then it is termed abused. Today there are very many drugs that are being used for sheer feeling of euphoria the users derive from them. These drugs are common in streets needless to mention some of the drugs that are used in hospitals for medicinal purposes have also been abused greatly. When a particular drug is used for quite a long time for non-medical purpose it becomes very toxic to the body. Substance abuse is a vice that needs to be fought at all costs and from all fronts as it has opened avenues through which lives have been lost. The problems that a person can suffer from long-term drug abuse spring from all the dimensions of a person’s health be it psychological health, mental health, physical health as well as his social relations. A person who is a victim to drug abuse may fail to cater for family needs, school obligations and even fail to have peace within him as he will be having lots of personal and interpersonal conflicts. Drug and substance dependence is commonly known as addiction. Drug or substance dependence is characterized by change in behaviors of a person. Most common behavior being the need to use more quantities of the substance. When a person is dependent on a given substance his life begins to revolve around it and it seems rather hard for him to live without using the substance. The person often suffers such symptoms as withdrawal among other symptoms associated with drug abuse and dependence.

Drug abuse and dependence are dangerous for an individual; however when a person has just began using a particular substance he may be easily helped to quit the habit than when he has used it for so long that he has become dependent on the drug and has begun showing those side effects that are associated with drug dependence. It is also good to note that a person may become dependent on a drug without abusing it. It is also good to note that person may abuse substance for quite a long time without ‘graduating’ to drug dependence.

One of the drugs that are being abused today is the Ketamine. Ketamine is one of the drugs that are very useful in hospitals. It is a perfect example that even some drugs that help us in gaining good health can also be abused. Ketamine is a medication that has been used to treat many illnesses. It is used in medical procedures with humans and other animals and that means it is an accepted medication in hospitals hence can be easily accessed by medical practitioners such as nurses and doctors. In hospitals it is mainly for starting and maintaining general anesthesia especially in scenarios where the patient is to go through intense pain. It also has other uses and these include sedation in intensive care, as a pain killer. It is however commonly used as a painkiller in emergency cases when the patient is allergic to other known drugs used in suppressing pain such as opiate drugs. This drug can be used as treatment of bronchospasm, and as a treatment for complex regional pain syndrome.

Ketamine has been found to work better since its administration does not affect the Respiratory function. For this reason it has become a very valuable anesthetic. However one of the known side effects often associated with administration of ketamine is agitation.

Ketamine is a NMDA noncompetitive Receptor antagonist

Ketamine is an arylcyclohexylamine derivative of phencyclidine. It is also a non-competitive NMDA antagonist. Scientist, Lodge and his colleagues the first showed that ketamine, phencyclidine, related arylcyclohexylamines and congeners were antagonists of excitatory amino acids like aspartate and glutamate in 1983. The early history of the development of ketamine as an anesthetic agent was documented by McCarthy in 1981. Other scientists Corssen and Dundee reviewed the historical introduction of ketamine into human anesthesia and the term dissociative anesthesia in 1990. These scientists found that for ketamine to be used safely in clinical therapies, it had to be tamed.

Low doses of ketamine in humans do not necessarily alter perception in a negative way. Foster gave an IV infusion of three different sub anesthetic doses of ketamine (0.05, 0.1 and 0.2 mg/kg/h) to six patients with Alzheimer’s disease. The patients showed no drowsiness and their reaction times and digit span were unaffected by any of the doses of ketamine used. This study however is rather controversial. This is because NMDA receptors are involved in brain function, including arousal and memory, this study requires further research and explanation because one would have predicted exactly the opposite effects even with the small doses of ketamine used.

Ketamine Intoxication

Ketamine as nicotinic inhibitor

Initially the effect of ketamine blockade on niconitic receptors was unknown. But today after many researches and experiments scientists have shown that racemic ketamine and the isomers inhibits nAChRs and K channels in a concentration-dependent and reversible manner. In an experiment racemic ketamine inhibited nAChRs and K channels, with the anesthetic concentration inducing the half-maximal effect being 1.4 and 300 micrometer, respectively. Only inhibition of the nAChRs was stereo selective. The half-maximal concentrations were 0.8 and 3.6 micrometer for S (+) – and R (-)-ketamine. The K channels were 350 and 70 times less sensitive to the effects of S (+) – and R (-)-ketamine.

Ketamine at concentrations found during clinical anesthesia exerts stereospecific effects on human ganglionic nAChRs but not on voltage-dependent K channels. The results found from this experiment supports the view that ketamine impairs sympathetic ganglionic transmission. Nonspecific effects on voltage-dependent K channels may underlie psychomimetic side effects.

Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.

Ketamine Intoxication Abuse and Dependence

Dextromethorphan (DXM) As a Drug of Abuse

September 25, 2014

Dextromethorphan (DXM) As a Drug of Abuse

Dextromethorphan (DXM) As a known fact, most of the drugs that are now commonly abused began as clinical drugs. There are clinical drugs that might have recreational properties in that when a person takes more than recommended dosage he may experience some of the effects of the drug. These may include hallucination and euphoria. For this reason these drugs can be misused in large scale if measures are not taken to strictly regulate their use. Dextromethorphan is one of the drugs that have been used in clinical setup but are known to be rich in recreational properties.

Dextromethorphan (DXM) was used as a cough depressant in the past. Most of the over the counter cough medicines has it as an ingredient. It works in these drugs as an antitussive (cough suppressant) and expectorant in other words it works as an agent that promotes the removal of mucus from the respiratory tract. It also has other medical uses. These may include the temporary relief of sinus congestion, runny nose, cough, sneezing, itching of the nose and throat, and watery eyes caused by hay fever, allergies, cold, or flu (influenza). In fact most of the over the counter cough medication has DXM as the most active component. When the recommended dose is taken, DXM has few adverse side effects, and has a long history of safety and effectiveness. However when taken in huge doses beyond the description it has some serious side effects. It causes hazy images and poor vision plus it also causes hallucinations. This drug, owing to its hallucinatory effects has been highly abused.

Over the past few years, cases related to use of DXM for non-medical purposes has risen and still very many people are using this drug for all the wrong reasons. Experts opine that the rise in abuse of this drug is attributed to the ease of purchasing nonprescription cough drugs from drug stores and in the internet. The drug is also legal and so even those who use it for wrong purpose are not afraid of the authorities even if they are found to be in possession of DXM. This gives it a more reason to be used as opposed to other hallucinogens that are considered illegal in most states. The FDA approves the use of DXM for medicinal purposes basing on the fact that when it is used within the prescribed doses then it can not cause any health hazard. However, it can be a damaging substance. Recreational users intentionally exceed suggested doses to experience a sense of heightened perceptual awareness, altered time perception, and/or visual hallucinations. Also, users often abuse the drug in combination with other drugs. The interaction between DXM and other substances e.g., alcohol, acetaminophen, MDMA/ecstasy, and other OTC cough medicines. When DXM is used with other drugs for recreational purposes, it produces a synergistic effect that can be very dangerous. Ingredients of cough medicines other than DXM, like acetaminophen, are extremely hazardous when consumed in high doses and can cause liver damage, heart attack, stroke, and death. For these reasons it is very important to restrict oneself to the prescribed dosage to avoid all the other undesirable effects.

DXM as Sigma receptors agonists

This drug works in a number ways in suppressing coughs. Firstly it has pharmacodynamic similarities to the N-methyl-D-aspartate (NMDA) receptor antagonist ketamine. It is used as a cough depressant as it has been found to be effective yet very safe when used within the required doses. However this drug does not bind on the N-methyl-D-aspartate (NMDA) receptors only but also binds to sigma-1 (σ1) receptors, which are believed to be protein targets for a potential new class of antidepressant medications.

Due to its hallucinatory effects it has become abused in that instead being used for medicinal purposes people now use it as a recreational drug. When taken a person will experience visual hallucinations and radically altered states of consciousness, often experienced as pleasurable and illuminating. This intense feeling of happiness and euphoria is what make many people to abuse DXM. It takes a person to a mental trip where every boundary of the mind seems overcome. However in case of overdose with the good feelings of happiness and euphoria a person may get feelings of anxiety and revulsion after using DXM. However there are other side effects associated with it.

Dextromethorphan (DXM)

Dextromethorphan side effects

Every drug has a side effect when abused. However the drugs will induce different reactions in people. As for DXM, it is very safe when used within the prescribed doses. However when a person uses this drugs in higher doses he will have to go through certain problems that are induced by the drug. There is however an innocent unintentional overdose under which a person may suffer such symptoms as; difficulty breathing, swelling of your face, lips, tongue, or throat. When this happens, you should stop using dextromethorphan and call your doctor at once if you have any of these serious side effects: severe dizziness, anxiety, restless feeling, or nervousness, confusion, hallucinations and slow, shallow breathing.

Apart from the unintentional overdose that may be termed accidental a person may overdose to get the feelings of euphoria and hallucinations from this drug. However this may result in serious health problems both short-term and long-term.

Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.

Dextromethorphan (DXM) As a Drug of Abuse

Phenethylamine Analogues and Addiction

September 24, 2014

Phenethylamine Analogues Are Potentially Addictive

Phenethylamine Amphetamine was used to treat children with attention deficit disorder until its addictive potential was recognized. The fact that it could be abused led the physicians to do lots of research in order to come up with its substitute in medical field that did not have much adverse effects. However to the youths amphetamine has become a substance of abuse that many are familiar with. Here are details of the experiments, the substitutes or other the amphetamine analogues and how they work.

In an experiment Methylphenidate was found to inhibit competitively the striatal dopamine transporter (DAT) and bind at sites on the DAT in common with both cocaine (a non-substrate site ligand) and amphetamine (a substrate site ligand). Some methylphenidate analogues modified on the aromatic ring or at the nitrogen were tested to determine whether the profile of inhibition could be altered. None was found to stimulate the release of dopamine in the time frame of 60 seconds of the experiments conducted, and each of the analogues tested was found to noncompetitively inhibit the transport of dopamine. It was found that halogenating the aromatic ring with chlorine (threo-3, 4-dichloromethylphenidate hydrochloride; compound;

1) Increased the affinity of Methylphenidate to inhibit the transport of dopamine. A derivative of Methylphenidate with simultaneous, single methyl group substitutions on the phenyl ring and at the nitrogen (threo-N-methyl-4-methylphenidate hydrochloride; compound

2) Bound at a site in common with Methylphenidate. A benzyl group positioned at the nitrogen (three-N-benzylmethylphenidate hydrochloride; compound

3) Imparted properties to the inhibitor in which binding at substrate and non-substrate sites could be distinguished. This analogue bound at a mutually interacting site with that of methylphenidate and had a Kint value of 4.29 mM. Furthermore, the N-substituted analogues (compounds 2 and 3), although clearly inhibitors of dopamine transport, were found to attenuate dramatically the inhibition of dopamine transport by amphetamine, suggesting that the development of an antagonist for substrate analogue drugs of abuse may be possible.

Phenethylamine Methylphenidate is currently the most commonly prescribed drug to treat children with attention deficit disorder and is also used to treat narcolepsy. Originally, amphetamine was used to treat children with attention deficit disorder until its addictive potential was recognized. It was estimated in 1992 that 3% of school age children were being treated with Methylphenidate for some extended interval. These numbers have continued to increase. Methylphenidate is not thought to stimulate dopamine synthesis or induce release of dopamine from nerve terminals. The action of Methylphenidate is to block the inward transport of dopamine into the presynaptic terminal, resulting in a prolonged dopamine stimulus.

Although Methylphenidate, a psychomotor stimulant agent, has been shown to have abuse potential, it is still the drug of choice for the treatment of children with attention deficit disorder. Methylphenidate has been shown to bind at the dopamine transporter (DAT) and its binding is saturable and specific for the DAT but it is not clear where Methylphenidate binds on the transporter relative to dopamine and other inhibitors of transport.

Methylphenidate is thought to have behavioral, pharmacological, and binding properties similar to those of amphetamine. Therefore, Methylphenidate has been classified as a non-transported inhibitor of DAT as well as a substrate analogue for DAT when present at high concentrations these discrepancies have led to the current study, which focuses on comparing the inhibition properties and binding sites of Methylphenidate with those of some Methylphenidate structural analogues, amphetamine, and cocaine. The results of previous work by this laboratory in a kinetic model of the actively transporting DAT have shown that amphetamine and m-tyramine bind to the same site on the DAT and at a site competitive with dopamine .Thus, it was shown that amphetamine and m-tyramine are substrate analogues for the DAT. It was shown that amphetamine binds at a site that is separate but interacting with the inhibitory site of cocaine on the DAT.

Different Methylphenidate derivatives have been synthesized in an attempt to develop compounds that will block cocaine binding to the DAT but do not interfere with substrate binding or transport. The test used for their assessment has been to compare the IC50 for inhibition of the transport of dopamine with the IC50 of the test analogue for the displacement of [3H] WIN 35,428 binding.

In this current study, amphetamine, cocaine, and selected structural analogues of Methylphenidate were used to decipher whether Methylphenidate resembles amphetamine or cocaine in its effects on the function of DAT. The Methylphenidate derivatives studied in this work were chosen for their particular characteristics. Compound 1, a dichloro-substituted derivative, is one of the more potent Methylphenidate derivatives with respect to inhibition of [3H] WIN 35,428 binding. It differs from most other Methylphenidate derivatives that have been synthesized in that it is equipotent as an inhibitor of [3H]WIN 35,428 binding and [3H]DA uptake and it also has an equilibrium Hill coefficient (nH) determined against [3H]WIN 35,428 binding of dopamine. Most of the other Methylphenidate analogues are at least threefold less potent as inhibitors of [3H] DA uptake and have nH values of unity. Compounds 2 and 3 were included because they are some of the most effective analogues in discriminating between [3H] WIN 35,428 binding and [3H] DA uptake, with a five- to sevenfold separation in potency to inhibit binding versus transport.

Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.

Phenethylamine Analogues Are Potentially Addictive

Hallucinogens? What Are They?

September 23, 2014

Widely Used Hallucinogens

There some drugs that when used may cause hallucinations. The drugs that cause hallucinations are called hallucinogens. These drugs when taken make a person to see things that are not even in existence. The drugs take a person to a trip. He ceases to see what is in the real world but instead sees things that nobody else sees. Hallucinogens may also have other destructive effects to those who take then in fact most drugs that cause hallucinations are often linked to such grave symptoms as memory loss among others. Hallucinogens are interesting drugs, they work differently for each individual person. A person may take a hallucinogen in huge quantity but still will not see many crazy visual hallucinations as compared to others who will even see dogs talk to him in his hallucinations even after taking the least quantities available.

hallucinogens

I’ve never actually taken LSD before but i know and have talked with many people who have. Color enhancement, visual distortions, and “melting” are typical effects produced by LSD in medium quantities. One of the drugs that cause a person to hallucinate is the LSD. The way LSD affects people varies greatly, however when taken it can take you to a ‘trip’ that may go for as long as 12 hours but there is a peak halfway through the middle. During these trips a person may also experience bodily changes which include dilated pupils, increased blood pressure and a high body temperature. People on LSD may also feel dizzy, sweat, have blurred vision and feel tingling in their hands and feet. They may feel drowsy but not sleepy.

LSD also induces a feeling of euphoria and a person becomes extremely happy laughs a lot and everything in his world becomes magically beautifully. A person who has taken LSD will feel like he has broken the barriers of his brain and hence become very contemplative. They feel like they have learnt new ways that were hidden and they get new understanding of how things are in the world. They trip to religious and spiritual a journey which is dreamlike revealing very strange phenomena to them. The colors in their surrounding become stronger than they really are and so are the lights that become brighter than normal. Taking LSD also causes synesthesia — a confusion of sensations between different types of stimuli. Some people have described this as seeing colors when they hear specific sounds.
LSD also causes poor judgment and so LSD users prefer taking the drug in groups and in calm environments like homes where they may not interact with other people who may take advantage in the twist of their judgment. They may spend a better part of their trip trying to understand something that seems rather unimportant.

Sometimes a person may have to be taken to hospitals in case he has got ‘a bad trip’ which means he might be hallucinating to a point not good for his mental health. The trip may take too long and in most instances the person may lose control. When taken to hospital he may be injected with anti-anxiety medication or a mild tranquilizer to ease the patient’s panic.

Mescaline

hallucinogens Mescaline is a naturally occurring psychedelic found in several cactus species, most notably, Peyote (Lophophora williamsii) and San Pedro (Trichocereus pachanoi). Several other members of the trichocereus family also contain mescaline.
Mescaline belongs to a family of compounds known as phenethylamines, making it quite distinct from the other major psychedelics which belong to the indole family. LSD, psilocybin, harmaline, and DMT are all indoles. Many synthetic “designer” psychedelics, such as ecstasy (MDMA) and 2C-B, are phenethylamines, and are related to the chemistry of mescaline.

Mescaline has been used for a long time in religious functions in san Pedro and today the use of mescaline in religious functions is still upheld by the Peru. The major reason why this plant extract is being used in for religious purposes is because of the hallucinatory effects it possesses. It helps a person to see more than he could in normal setting.

Due to its hallucinatory effects it has become abused in that instead being used for religious purposes people now use it as a recreational drug. When taken a person will experience visual hallucinations and radically altered states of consciousness, often experienced as pleasurable and illuminating. It takes a person to a mental trip where every boundary of the mind seems overcome. However with the good feelings of happiness and euphoria a person may get feelings of anxiety and revulsion after using mescaline. Visualizations euphoria and laughter are the better part of taking mescaline. However there are other side effects associated with it.

Side effects of mescaline

Being a product highly valued as it is used for religious purposes most researches that have been done on it have not shown its side effects. However these are the side effects that have been reported; dizziness, anxiety, increased heart beat diarrhea and even headache. However vomiting is considered an advantage by the Shaman ceremonies as it is considered cleansing.

Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.

Category Archives: Preceptorship Addiction Treatment

New and re-emerging Abused Drugs

New and re-emerging Abused Drugs