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PubMed1976

Comparison of behavior maintained by infusions of eight phenylethylamines in baboons.

Doses of eight phenylethylamines were substituted for cocaine on a drug-maintained behavior baseline in baboons. Intravenous infusions of drug were contingent upon completion of 160 lever presses (a 160-response fixed-ratio schedule; FR 160). A 3-h time-out period followed each infusion, permitting a maximum of 8 infusions per day. Fenfluramine was the only drug that did not maintain self-infusion performance at any dose tested. d-Amphetamine was approximately 10 times more potent than phentermine, phenmetrazine or diethylpropion, and 20 to 30 times more potent than methylenedioxyamphetamine (MDA), clortermine or chlorphentermine, in maintaining self-infusion behavior. Some doses of d-amphetamine and phentermine produced a cyclic pattern of drug intake over days. Increasing self-infused doses of all drugs produced a substantial suppression of concurrent food-maintained behavior. There was no clear relation between the potency of the phenylethylamines in maintaining self-infusion performance and the potency in suppressing food-maintained behavior which indicates that different mechanisms may underlie the two effects. Examination of chemical structures indicates that substitution on the phenyl ring may decrease the potency of phenylethylamines in maintaining self-infusion behavior.

3,4-Methylenedioxyamphetamine↗
PubMed1977

Effects of antenatal exposure to anorectic drugs.

In a large prospective, observational study of pregnancy and child development, the anorectic drugs (amphetamines and phenmetrazine) prescribed to gravid women during different stages of pregnancy were evaluated for their teratogenicity. The severe congenital anomaly rate (SCA) per 100 live-born children at age five years did not differ from the SCA rate of the group of children whose mothers did not use these drugs. There was, however, an excess of oral clefts in the offspring of mothers who had amphetamines prescribed in the first 56 days from the last menstrual period. A rought test of efficacy of anorectic drugs by comparing mean weight gains in four-week periods before and after the prescription showed only short-term and limited reduction of weight gain.

Abnormalities, Drug-Induced↗
PubMed1975

Simultaneous detection of a wide variety of commonly abused drugs in a urine screening program using thin-layer identification techniques.

A single-step extraction method and thin-layer identification techniques capable of testing a wide variety of drugs of abuse are presented. These techniques are well suited for large and/or small drug programs involved in urine testing because they provide substantial economic benefits and improve clinical functioning. The drugs are absorbed on a 6 X 6 cm piece of paper loaded with cation-exchange resin and then eluted from the paper at pH 10.1 using ammonium chloride-ammonia buffer. The simultaneous thin-layer detection of sedatives, hypnotics, narcotic analgesics, central nervous system stimulants and miscellaneous drugs is accomplished by spotting the solution of extracted residue on a 20 X 20 cm Gelman pre-coated silica gel glass microfiber sheet (ITLC Type SA). A two-stage solvent system is used in order to obtain a chromatogram with optimum separation of a wide range of drugs. This system can separate methadone and/or cocaine from propoxyphene, methaqualone, methylphenidate, pentazocine, pipradrol, Doxepin, chlorpromazine, phenazocine, naloxone, naltrexone, imipramine and trimeprazine; amphetamine from phenylpropanolamine and dimethyltryptamine; codeine from dextromethorphan; methamphetamine from dimethyltryptamine, etc. Different detection reagents are then applied in succession to different marked areas of the developed chromatogram. This elegant method of extraction and spraying has enabled us to detect morphine base at a sensitivity level of 0.15 mug/ml, amphetamine sulfate at 1.0 mug/ml, methamphetamine hydrochloride at 0.5 mug/ml, phenmetrazine hydrochloride at 0.5 mug/ml, codeine phosphate at 0.5 mug/ml, methadone hydrochloride at 1.0 mug/ml, secobarbital at 0.36 mug/ml and phenobarbital at 0.5 mug/ml in urine. The minimum volume of urine needed to achieve these sensitivities is 20 ml. The cost of analysis per urine specimen using these techniques for concomitant screening of these drugs is less than US$ 1.

1-Propanol↗
PubMed1977

Comparative metabolism of the amphetamine drugs of dependence in man and monkeys.

The use of animal models to study drug dependence and tolerance requires that the species used metabolizes the drugs like man, a condition frequently not fulfilled by non-primate species. The metabolic fate of several amphetamine drugs, namely amphetamine, norephedrine, chlorphentermine and phenmetrazine, in the rhesus monkey and the tamarin and two non-primate species has been investigated and compared to that found for man. The findings show that the two primate species metabolize these drugs in a manner similar to that in man.

Amphetamines↗
PubMed1977

Rhabdomyolysis and shock after intravenous amphetamine administration.

Five patients who had injected intravenous (i.v.) phenmetrazine or methamphetamine developed marked prostration resembling septic shock, disseminated intravascular coagulation, rhabdomyolysis with myoglobinuria, and azotemia. Soon after injection, four noted chills, fever, sweats, nausea, and abdominal cramps. Within hours, they developed vomiting, myalgias, paresthesias, headache, and orthostasis. Cardiorespiratory arrest, accelerated bleeding, and noncardiac pulmonary edema were observed in one patient. From 4 to 11 litres of saline were required in the first 24 h to maintain blood pressure and urine output, suggesting that shock resulted from massive loss of intravascular volume into necrotic muscle. Recognition of this syndrome and treatment by aggressive volume replacement led to the recovery of all five patients.

Adult↗
PubMed1986

Arousal and stability: the effects of five new sympathomimetic drugs suggest a new principle for the prevention of space motion sickness.

Sympathomimetic agents are frequent components in antimotion-sickness drug combinations because of their usefulness in counteracting the sedation caused by stressful motion or resulting from the administration of other antimotion-sickness drugs. The noradrenergic neurochemistry of the brain's arousal-attentional systems prompted us to evaluate the efficacy of five new sympathomimetic drugs and to further define the role of arousal in susceptibility to motion. Subjects were orally administered methamphetamine (20 mg), phenmetrazine (25 mg), phentermine (37.5 mg), methylphenidate (20 mg), or pemoline (75 mg) 2 h prior to taking a Staircase Profile Test. All of the drugs increased resistance to stressful coriolis stimulation by 80-120%. Methylphenidate and pemoline showed fewer side effects. These findings, interpreted in conjunction with the documented inefficacy of most anticholinergic and antihistaminergic drugs tested to date, suggest that sympathomimetic drugs or a generalized state of arousal can inhibit the development of motion sickness.

Clinical Trials as Topic↗
PubMed1976

Characteristics of unlimited access to self-administered stimulant infusions in dogs.

When drug-naive dogs were given unlimited access to response-contingent intravenous infusions of either d-amphetamine, phenmetrazine, or methylphenidate, a regular cycle of drug intake interspersed with periods of voluntary abstinence was seen. During the drug self-administration phases there was a marked increase in locomotor behavior and stereotypy along with a decrease in body weight; the rest periods were characterized by minimal activity. These results are similar to those observed when humans engage in high-dose intravenous abuse of psychomotor stimulants.

Animals↗
PubMed1998

Drugs and colon cancer.

In a case-control study of colon cancer conducted in three geographic regions of the United States, 1993 case subjects and 2410 control subjects were interviewed. In addition to queries regarding other known or suspected risk factors, subjects were asked about their use of eight drugs or drug groups. Two of these, aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs), have been inversely associated with risk in other studies. Three others--asthma medications, digitalis preparations, and phenmetrazine--were positively associated and the last three--diazepam, penicillin, and phenformin--were negatively associated with risk of colon cancer in an earlier study that screened pharmaceuticals for possible carcinogenic effects. Reported use of aspirin and NSAIDs were both inversely related to risk with essentially the same odds ratios (0.7, 95% confidence interval 0.6-0.8) for both drugs in both univariate and multivariate analyses controlling for use of each other and for other colon cancer risk factors. Subdivision by age at starting the drug, duration of use, latency interval, sex, race, family history of colon cancer, or proximal versus distal cancer revealed no substantial differences among subgroups for either aspirin or NSAIDs, but reduced risk was associated primarily with recent aspirin use. Phenformin showed a strong positive association but the data concerning this drug appeared to be inaccurate. The other drugs and drug groups showed essentially no association with colon cancer risk.

Journal Article↗
PubMed2000

Drugs for nocturnal enuresis in children (other than desmopressin and tricyclics).

BACKGROUND: Enuresis (bedwetting) is a socially unacceptable and stressful condition which affects around 15-20% of five year olds, and up to 2% of young adults. Although there is a high rate of spontaneous remission, the social, emotional and psychological costs to the children can be great. OBJECTIVES: To assess the effects of drugs other than desmopressin and tricyclics on nocturnal enuresis in children, and to compare them with other interventions. SEARCH STRATEGY: The following electronic databases were searched: MEDLINE to June 1997; AMED; ASSIA; BIDS; BIOSIS Previews (1985-1996); CINAHL; DHSS Data; EMBASE (1974 to June 1997); PsycLIT and SIGLE. Organisations, manufacturers, researchers and health professionals concerned with enuresis were contacted for information. The reference sections of obtained studies were also checked for further trials. Date of the most recent search: July 1997. SELECTION CRITERIA: All randomised trials of drugs (excluding desmopressin or tricyclics) for nocturnal enuresis in children were included in the review. Trials were eligible for inclusion if: children were randomised to receive drugs compared with placebo, other drugs or other conservative interventions for nocturnal bedwetting; participants with organic causes for their bedwetting were excluded; and baseline assessments of the level of bedwetting were provided. Trials focused solely on daytime wetting were excluded. DATA COLLECTION AND ANALYSIS: Two reviewers independently assessed the quality of the eligible trials, and extracted data. MAIN RESULTS: None of the drugs (phenmetrazine, amphetamine sulphate/ephedrine + atropine, furosemide (sic) or chlorprotixine) were better than placebo during treatment. The numbers were too small to draw reliable conclusions, and none are used in current practice in the UK. Imipramine (a tricyclic) was better than each of the three drugs with which it was compared (meprobamate, ephedrine sulphate and furosemide) even though the numbers were small. Alarm treatment was better than drugs in one small trial. REVIEWER'S CONCLUSIONS: There was not enough evidence to suggest that the included drugs reduced bedwetting. There was limited evidence to suggest that imipramine and alarms were better, and in other reviews, desmopressin, tricyclics and alarm interventions have tentatively been shown to be effective.

Child↗
PubMed2005

Pharmacotherapy for weight loss in adults with type 2 diabetes mellitus.

BACKGROUND: Obesity is closely related to type 2 diabetes and long-term weight reduction is an important part of the care delivered to obese persons with diabetes. OBJECTIVES: To assess the efficacy of pharmacotherapy for weight loss in adults with type 2 diabetes. SEARCH STRATEGY: Computerized searches were performed of MEDLINE (January 1966 to May 2004), EMBASE (January 1974 to May 2004, Web of Science (January 1981 to May 2004, and other electronic bibliographic databases, supplemented with hand searches of reference lists and selected journals. SELECTION CRITERIA: Randomized, controlled trials were included where pharmacotherapy was used as the primary strategy for weight loss among adults with type 2 diabetes. Published and unpublished literature in any language and with any study design was included. DATA COLLECTION AND ANALYSIS: Two reviewers abstracted data and the quality of included studies was evaluated by assessing potential attrition, as well as selection and measurement bias, and a Jadad score was obtained. Effects were combined using a random effects model. MAIN RESULTS: A sufficient number of studies were available for a quantitative synthesis for fluoxetine, orlistat, and sibutramine. Twenty two randomized controlled trials were included in the review, with a total of 296 participants for fluoxitine, 2036 for orlistat, and 1047 for sibutramine. Pharmacotherapy produced modest reductions in weight for fluoxetine (5.1 kg (95% confidence interval [CI], 3.3 - 6.9) at 24 to 26 weeks follow up; orlistat 2.0 kg (CI, 1.3 - 2.8) at 12 to 57 weeks follow-up, and sibutramine 5.1 kg (CI, 3.2 - 7.0) at 12 to 52 weeks follow-up. Glycated hemoglobin also modestly and significantly reduced for fluoxetine and orlistat. Gastrointestinal side effects were common with orlistat; tremor, somnolence and sweating with fluoxetine; and palpitations with sibutramine. Some studies, using a variety of study designs, were available on other drugs and a significant decrease in weight was noted in three studies of mazindol, one of phenmetrazine, two of phentermine. No studies were identified that fit inclusion criteria for pseudophedrine, ephedra, sertraline, yohimbine, amphetamine or its derivatives, bupropion, topiramate, benzocaine, threachlorocitric acid, sertraline, and bromocriptine. AUTHORS' CONCLUSIONS: Fluoxetine, orlistat, and sibutramine can achieve statistically significant weight loss over 12 to 57 weeks. The magnitude of weight loss is modest, however, and the long-term health benefits remain unclear. The safety of sibutramine is uncertain. There is a paucity of data on other drugs for weight loss or control in persons with type 2 diabetes.

Adult↗
PubMed1978

Analysis of feeding suppression produced by perifornical hypothalamic injection of catecholamines, amphetamines and mazindol.

The effects on feeding of perifornical hypothalamic injection of catecholamines, amphetamines and mazindol were examined in hungry rats. In pargyline-pretreated subjects, both dopamine and epinephrine significantly suppressed food intake, at doses as low as 31 ng for dopamine and 150 ng for epinephrine (the latter injected with an alpha-adrenoceptor blocker). This effect was reliably strengthened by inhibiting catecholamine deamination or presynaptic catecholamine uptake. Perifornical injections of amphetamine, mazindol, methamphetamine, and phenmetrazine also suppressed feeding. The magnitude of this effect in individual animals was positively correlated with the effect produced by catecholamine agonists. Moreover, this effect of mazindol was partially antagonized by perifornical injection of dopaminergic and beta-adrenoceptor blockers. The effects of amphetamine and epinephrine were abolished by these drugs, while dopamine's effect was selectively inhibited by the dopaminergic antagonist. Serotonergic antagonists produced no change. These findings lend support to the hypothesis that perifornical hypothalamic catecholamine neurons, through dopaminergic receptors and beta-adrenoceptors, are involved in inhibiting feeding behavior, as well as in mediating the anorexic action of the amphetamines and mazindol.

Amphetamines↗
PubMed1986

Differential effects of amphetamine and related compounds on locomotor activity and metabolic rate in mice.

Locomotor activity was measured by photobeam interruptions, and metabolic rate by the production of CO2 (as minute volume expired CO2, or VECO2) in mice. d-Amphetamine (0.3 to 10 mg/kg IP) increased locomotor activity in a dose-dependent manner while suppressing VECO2 over the same 72-min test period, compared to saline-injected controls. This phenomenon of divergent effects on locomotor activity and metabolic rate required central stimulation, as neither ammonium sulfate nor p-hydroxyamphetamine suppressed VECO2. Oxygen consumption was also suppressed by d-amphetamine, indicating that the suppression of VECO2 involved more than a change in respiratory quotient. When baseline activity rates were increased with running wheels, VECO2 and activity were both suppressed by d-amphetamine; VECO2 was suppressed by d-amphetamine more in exercising mice than in sedentary mice. Anorexigenic agents phenmetrazine, aminoxaphen, and fenfluramine, when administered in doses equimolar to maximally effective doses of d-amphetamine, did not consistently affect activity or VECO2. Evidence for mediation of the VECO2 response by corticosterone and endogenous opioid peptides was negative. Further work, with other mediators of the stress response, or with more complete dose-effect studies with anorexigenic compounds, may be necessary to explicate the mechanism of this counter-intuitive divergence of two measures of activity in mice.

Adrenocorticotropic Hormone↗
PubMed1990

Three-choice discrimination among (+)-amphetamine, fenfluramine and saline in pigeons.

Five pigeons were trained to discriminate among (+)-amphetamine (AMPH; 1.7 or 3.0 mg/kg), fenfluramine (FEN; 5.6 or 10 mg/kg), and saline using a three-choice drug discrimination procedure. The results of the study demonstrated that a reliable discrimination between AMPH and FEN could be obtained and the discriminative stimulus (DS) effects of these two drugs did not overlap, i.e., were mutually exclusive. Phenmetrazine produced a dose-related increase in AMPH-appropriate responding with no responding occurring on the FEN-appropriate key. Two serotonin agonists, quipazine (5-HT2) and MK 212 (5-HT1), produced FEN-appropriate responding in two of three pigeons, while a third pigeon responded predominantly on the AMPH-appropriate key following their administration. In contrast, phencyclidine produced predominantly (greater than 50%) saline-appropriate responding, indicating that the DS effect of phencyclidine was unlike either AMPH or FEN. Finally, compounds known to have multiple DS properties such as MDA and MDMA were tested. The results with these compounds confirmed that these drugs have complex DS effects both within and across individual pigeons.

3,4-Methylenedioxyamphetamine↗
PubMed1986

Propylhexdrine.

Propylhexedrine, a sympathomimetic with varied medicinal uses, is one of the compounds to be reviewed by the Expert Committee convened by the World Health Organization (WHO) to determine whether the compound should be scheduled under the Convention on Psychotropic Substances. This paper reviews the pharmacology, medicinal uses, toxicity and abuse-potential of propylhexedrine, with special emphasis on toxicity and abuse potential. The primary medicinal use of propylhexedrine is temporary symptomatic relief of nasal decongestion due to colds, allergies and allergic rhinitis. When used as a nasal inhaler for this indication, propylhexedrine reduces nasal airway resistance without producing rebound congestion. Abuse does not occur by nasal inhalation; however, a small amount of abuse of the propylhexedrine containing nasal inhalers occurs by oral ingestion of the contents of the inhaler or by intravenous injection. Propylhexedrine is a central nervous system (CNS) stimulant of low abuse potential, a stimulant of low preference for stimulant abusers compared with amphetamine, methylphenidate, phenmetrazine.

Adult↗
PubMed1984

Some new urinary metabolites of famprofazone and morazone in man.

The human urinary metabolism of two pyrazolone derivatives, morazone and famprofazone, has been investigated. After administration of morazone, the metabolites p-hydroxymorazone and phenazone-4-carboxylic acid were excreted in addition to the known metabolite, phenmetrazine, and unchanged morazone. Metabolism of famprofazone led to the formation of methamphetamine; the pyrazolone moiety was excreted as 3-hydroxymethyl-propyphenazone.

Journal Article↗
PubMed1979

Inhibition of 3H-dopamine accumulation in reserpinized and normal rat striatum.

The inhibitory potencies of 27 compounds on the accumulation of 3H-dopamine (DA) in synaptosome-rich striatal homogenates of normal and reserpinized rats were determined. It was found that some compounds, e.g. amphetamine derivatives, phenmetrazine, phenethylamine derivatives and tryptamine derivatives were considerably more potent in the reserpinized preparation than in the normal one. Other compounds, e.g. amfonelic acid, mazindol, EXP 561, benztropine, pipradrol, nomifensine, methylphenidate and cocaine had similar potencies in the two preparations. It is suggested that the compounds enhanced by reserpine are more potent as DA releasing agents than as inhibitors of the DA uptake, whereas the compounds in the other group are most potent as uptake inhibitors. Interestingly, these two groups completely agree with the two groups of central stimulatory agents, viz. the amphetamine-like and the methylphenidate-like drugs.

Amphetamines↗
PubMed1977

Biochemical differentiation of amphetamine vs methylphenidate and nomifensine in rats.

Amphetamine-like stimulants were divided into two groups, one in which the stereotyped behaviour was not antagonized by reserpine [(+)-amphetamine, (-)-amphetamine, methamphetamine, phenmetrazine and phenethylamine] and another group in which the behavioural effects were blocked by reserpine (methylphenidate, nomifensine, pipradrol and amfonelic acid (NCA; Win 25978)). Both groups increased homovanillic acid (HVA) in whole brain 2 h after administration. The 'methylphenidate group' also increased brain 3,4-dihydroxyphenylacetic acid (DOPAC) in naive rats; whereas the '(+)-amphetamine group' decreased DOPAC in naive rats, as well as in reserpinized rats, alpha-methyl-p-tyrosine-treated rats and after acute hemisection. The reserpine antagonism of the 'methylphenidate group'-induced stereotyped behaviour was partially reversed by type A monoamine oxidase inhibition. The '(+)-amphetamine group'-induced stereotyped behaviour was not blocked by short time pretreatment with alpha-methyltyrosine, only by longer pretreatment intervals. The mechanisms by which the two groups are differentiated biochemically is discussed with special attention to possible intra-neuronal inhibition of dopamine oxidation by the '(+)-amphetamine group'.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1992

Appetite suppressants. A review.

Centrally acting appetite suppressant drugs used in the treatment of obesity fall into 2 broad pharmacological categories; those which act via brain catecholamine pathways and those which act via serotonin pathways. Of the former group, amphetamine and phenmetrazine are no longer recommended because of their stimulant properties and addictive potential. The remaining drugs in this class include amfepramone (diethylpropion), phentermine, mazindol and phenylpropanolamine. All have been shown to reduce appetite and lower food intake, thereby helping obese patients more easily keep to a low-calorie diet and lose weight. They all have some sympathomimetic and stimulant properties. Anorectic drugs which promote serotonin neurotransmission have no such stimulant or sympathomimetic properties. They are fenfluramine, together with its recently introduced dextrorotatory stereoisomer dexfenfluramine, and fluoxetine. They reduce appetite and food intake and are effective in the treatment of obesity. Anorectic drugs should be reserved for those who are clinically at risk from being overweight, and then only as part of a comprehensive weight-reducing programme including regular dietary counselling. Although current licensing regulations only allow their use over a relatively short period (12 to 16 weeks), clinical trials have shown them to be effective over longer periods, particularly in preventing weight regain. Of the compounds currently indicated for use in obesity, dexfenfluramine appears to have the most suitable pharmacological profile, although it should not be given to patients with a history of depression. When used appropriately, appetite suppressants can be of real therapeutic benefit, and pose little risk.

Appetite Depressants↗