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At least 19 recordsLinked to original sources
PubMed2002

Biotransformation of cyclizine in greyhounds. 1: Identification and analysis of cyclizine and some basic metabolites in canine urine by gas chromatography-mass spectrometry.

1. The partial in vivo biotransformation of Marezine [(cyclizine.HCl); 1-diphenylmethyl-4-methylpiperazine hydrochloride] in the racing greyhound and the excretion of the unconjugated and conjugated (Phase II) basic metabolites of cyclizine in canine urine are reported. 2. Using copolymeric bonded mixed-mode solid-phase extraction cartridges, the basic isolates from both unhydrolysed and enzyme hydrolysed urine samples were isolated, derivatized as trimethylsilyl ethers and analysed by positive-ion electron ionization gas chromatography-mass spectrometry (EI(+)-GC-MS). Selected samples were analysed by positive-ion methane chemical ionization (CI(+))-GC-MS to aid structure elucidation of the putative metabolites. 3. Cyclizine was the major component excreted in post-administration urine. Five substrate-related basic compounds (M1--> M5) were tentatively identified by EI(+)- and CI(+)-GC-MS. The major Phase I metabolite was identified as norcyclizine [1-diphenylmethylpiperazine] (M1), the other metabolites (M2 --> M5) were tentatively identified as monohydroxylated products based on MS data. 4. Cyclizine and the N(4)-desmethyl metabolite (M1) are excreted unconjugated; the other four hydroxylated metabolites are excreted as Phase II conjugates (glucuronides and/or sulphates). Structures of the putative basic metabolites are presented. At least four other basic metabolites were also detected in post-administration urine, but could not be characterized from GC-MS data. 5. All unhydrolysed post-administration urine samples were analysed by selected ion monitoring EI(+)-GC-MS to quantify cyclizine and norcyclizine (M1) using authentic cyclizine as the analyte and chlorcyclizine as the internal standard. The level of M1 is expressed as 'cyclizine equivalents'. The duration of urinary elimination of cyclizine and M1 was obtained from their excretion profiles. 6. From these studies, cyclizine and norcyclizine (M1) would be the target compounds of choice in the development of screening and confirmatory methods for the detection of cyclizine administration to racing greyhounds. Information on any of the other metabolites may also be of some value for confirmatory analysis.

Animals↗
PubMed1977

Cyclizine-induced chorea. Observations on the influence of cyclizine on dopamine-related movement disorders.

Cyclizine was observed to induce generalized chorea in a patient with mild lingual-facial-buccal dyskinesias. The mechanism for this action was shown to be cyclizine's central anticholinergic activity. This was consistent with previous findings that acetycholine antagonists can lower the threshold for appearance of abnormal choreatic movements related to dopaminergic mechanisms by alteration of the dopamine/acetylcholine balance in the corpus striatum. Furthermore, our study was supportive of the hypothesis that spontaneous lingual-facial-buccal dyskinesias in the elderly may be the mildest manifestations of senile chorea.

Aged↗
PubMed1982

A comparison of triprolidine and cyclizine on histamine (H1) antagonism, subjective effects and performance tests in man.

1 The effects of triprolidine and cyclizine on the histamine skin response, performance tests and subjective effects were examined in a controlled, double-blind study in eight healthy volunteers. 2 Triprolidine was considerably more potent that cyclizine in inhibiting the skin response to histamine. Significant inhibition of flare size occurred at 1, 2 an 4 h after triprolidine 2.5 mg. A smaller but significant reduction occurred at 2 and 4 h after cyclizine 100 mg but not after the 50 mg dose. 3 Cyclizine 100 mg produced a significant increase in reaction time at 4.5 h compared with lactose. Smaller though non significant increases followed triprolidine and cyclizine 50 mg. 4 Subjective effects were seen only after cyclizine 100 mg when subjects were significantly more drowsy, feeble, muzzy, lethargic and dreamy than after lactose dummy. No significant changes followed triprolidine 2.5 mg or cyclizine 50 mg. 5 It was concluded that while cyclizine has antihistamine properties, these are weak compared with triprolidine, and are not seen with doses sufficiently low to avoid central nervous system impairment.

Adult↗
PubMed1997

Drug combinations in syringe drivers: the compatibility and stability of diamorphine with cyclizine and haloperidol.

The compatibility and stability of 2B combinations of diamorphine hydrochloride (5-100 mg/ml) with cyclizine lactate (5-50 mg/ml), eight combinations of diamorphine (10-100 mg/ml) with haloperidol (2-4 mg/ml) and eight combinations of all three drugs was assessed after storage in 1 ml polypropylene syringes. Samples were stored for periods up to seven days in the light and at room temperature (22 degrees C). Five combinations of diamorphine with cyclizine precipitated immediately upon preparation. After analysis and determination of t90% values (the time taken for 10% degradation). 16 of the remaining 23 combinations were judged to be compatible (no signs of crystallization or precipitation) and stable (less than 10% loss of potency of either drug) after storage for 24 h. After seven days storage only four remained compatible and stable. The results indicate that ratios of diamorphine to cyclizine of 1:1 are stable at concentrations up to 20 mg/ml. An increase in diamorphine concentration necessitates a reduction in cyclizine to 10 mg/ml, and an increase in cyclizine concentration necessitates a reduction in concentration of diamorphine to 15 mg/ml to maintain stability over 24 h. All the combinations of diamorphine with haloperidol remained compatible and stable for seven days. The addition of haloperidol (2 mg/ml) to the diamorphine and cyclizine combinations had no detrimental effect on their compatibility and stability. A stability curve is included as an easy way for palliative care personnel to avoid potential problems with incompatibilities and reduced stability when using these combinations. Furthermore, to reduce the possibility of precipitation with mixtures containing cyclizine, the use of 0.9% sodium chloride should be avoided.

Analgesics, Opioid↗
PubMed2003

Prevention of postoperative nausea and vomiting after spinal morphine for Caesarean section: comparison of cyclizine, dexamethasone and placebo.

BACKGROUND: Low-dose intrathecal (spinal) morphine (0.1-0.2 mg) for Caesarean section delivers excellent postoperative analgesia but is associated with significant nausea and vomiting. We compared the antiemetic efficacy of cyclizine, dexamethasone, and placebo in this clinical setting. METHODS: Ninety-nine women undergoing elective Caesarean section under spinal anaesthesia were allocated randomly, in a double-blind study design, to receive either cyclizine 50 mg, dexamethasone 8 mg, or placebo as a single-dose infusion in saline 0.9%, 100 ml on completion of surgery. Spinal anaesthesia consisted of: hyperbaric bupivacaine 0.5%, 2.0 ml; fentanyl 10 micro g; and spinal morphine 0.2 mg. The primary outcome measure was the incidence of nausea. RESULTS: The incidence of nausea was significantly less in patients receiving cyclizine compared with dexamethasone and placebo (33 vs 60 and 67%, respectively, P<0.05). Severity of nausea and number of vomiting episodes were also less at 3-6 h in cyclizine patients. Overall satisfaction with postoperative care at 24 h, expressed on a 100 mm visual analogue scale, was greater in cyclizine [78 (28)] than either dexamethasone [58 (31), P=0.03] or placebo [51 (28), P=0.008]. CONCLUSION: We conclude that following spinal morphine 0.2 mg and fentanyl 10 micro g analgesia for Caesarean section, cyclizine 50 mg i.v. reduces the incidence of nausea compared with dexamethasone 8 mg i.v. or placebo. It also lessens the severity of nausea and vomiting, and increases maternal satisfaction in the early postoperative period.

Adult↗
PubMed1989

Cyclizine abuse among a group of opiate dependents receiving methadone.

Twenty opiate dependents receiving long-term prescriptions of oral methadone, were identified as being habitual abusers of the anti-emetic drug cyclizine. A semi-structured interview elicited the dosage of cyclizine used, its effects, the reasons for starting and persisting with abuse of cyclizine and the attitudes of the patients to it. Cyclizine was taken in large doses intravenously with methadone. The effects initially were of intense stimulation, often with hallucinations, sometimes with aggressive behaviour, and occasionally with epileptic fits. Subsequent depressive mood changes occurred often accompanied by a craving for cyclizine. Tolerance to the drug occurred but no clear cut withdrawal syndrome is apparent. It seems that dependence upon cyclizine occurs. The significance of these findings for doctors, pharmacists and for drug treatment units is discussed. The paucity of information on the pharmacology and pharmacokinetics is noted.

Adult↗
PubMed2005

An LC-MS-MS method for the determination of cyclizine in human serum.

Cyclizine is a piperazine derivative with anti-emetic activity that is useful in the prevention and treatment of nausea and vomiting associated with motion sickness. A liquid chromatography-tandem mass spectrometry (LC-MS-MS) method is presented for the quantitation of cyclizine in serum. Sample pretreatment involved liquid-liquid extraction of 200 microl of serum with dichloromethane after the addition of 100 microl each of ammonium hydroxide and internal standard solutions. The extracts were analyzed by HPLC on a Luna C18 reversed-phase column and an ion-trap mass spectrometer with an electrospray interface. A limit of detection of 1 ng/ml was determined which allowed for the reliable measurement of cyclizine in the serum of human subjects. The method was found to be linear over the calibration range of 2.5-100 ng/ml. The applicability of this method was demonstrated by the analysis of serum obtained from a human volunteer following administration of a single 50 mg cyclizine hydrochloride tablet. The reported method was observed to have the necessary sensitivity, selectivity, precision and accuracy for monitoring cyclizine concentrations in human subjects following oral administration.

Calibration↗
PubMed2002

Comparison of cyclizine and ondansetron for the prevention of postoperative nausea and vomiting in laparoscopic day-case gynaecological surgery.

Seventy-four patients undergoing laparoscopic gynaecological surgery were randomly allocated to two groups receiving cyclizine 50 mg or ondansetron 4 mg at induction of anaesthesia. Anaesthetic and postoperative analgesia regimens were standardised. Approximately half of the patients in each group experienced some degree of postoperative nausea and vomiting (cyclizine, 56%; ondansetron, 54%). There was no difference between groups in respect of pre- and postdischarge incidence. Mean (SD) time to eye opening was significantly prolonged in the cyclizine group [10 (4) min vs. 8 (2) min; p < 0.001], but this had no influence on discharge times. Cyclizine and ondansetron appear equally effective in preventing postoperative nausea and vomiting but the 10-fold price differential favours cyclizine.

Adult↗
PubMed1999

Comparison of ondansetron and cyclizine for prevention of nausea and vomiting after day-case gynaecological laparoscopy.

We have compared ondansetron 4 mg i.v. and cyclizine 50 mg i.v., in a double-blind, randomized, placebo-controlled study for the prevention of postoperative nausea and vomiting (PONV) for 24 h after day-case gynaecological laparoscopy. Compared with placebo (n = 58), ondansetron (n = 60) and cyclizine (n = 57) reduced significantly the incidence of moderate or severe nausea (30% and 23% vs 52%; P = 0.02 and P = 0.001, respectively) and requirement for escape antiemetic (28% and 16% vs 47%; P = 0.04 and P < 0.001, respectively) before discharge from hospital. There were no significant differences in PONV after discharge. Significantly more patients suffered no PONV before and after discharge after ondansetron and cyclizine compared with placebo (31% and 33% vs 12%; P = 0.02 and P < 0.01, respectively). For diagnostic laparoscopy (n = 74), fewer patients received escape antiemetic after cyclizine than after ondansetron (4% vs 37%; P < 0.01); for laparoscopic sterilization (n = 101), both antiemetics were equally effective. Ondansetron and cyclizine both reduced severe and moderate nausea and the need for antiemetic therapy after day-case gynaecological laparoscopy.

Adult↗
PubMedDate not supplied

Cyclizine and droperidol have comparable efficacy and side effects during patient-controlled analgesia.

BACKGROUND: Post-operative nausea and vomiting (PONV) is common, especially following gynaecological surgery. Patient-controlled analgesia (PCA) is frequently complicated by nausea. We assessed PONV, pain and sedation in patients receiving cyclizine or droperidol during PCA following abdominal hysterectomy in a double-blind trial. METHODS: Thirty women were randomised to receive either cyclizine 0.7 mg/kg or droperidol 0.04 mg/kg during surgery followed by PCA containing morphine sulphate with cyclizine 2 mg or droperidol 0.05 mg per demand. Blinded observers scored levels of nausea, sedation, anxiety and pain. RESULTS: Pain scores, PCA usage and supplemental antiemetic requirements were comparable. Nausea and sedation scores were similar in both groups. Two patients in each group developed refractory PONV. Pre-operative anxiety scores were similar and decreased comparably over time. Patients developing refractory emetic sequelae had a higher incidence of previous PONV. Previous PONV also predicted lower PCA medication intake despite similar demand rates, suggesting increased usage during lock-out periods. CONCLUSION: Prophylactic cyclizine and droperidol have similar efficacy during PCA. Neither is associated with perioperative anxiety. A minority of patients have refractory PONV during PCA. Previous PONV may predict less efficient PCA usage.

Analgesia, Patient-Controlled↗
PubMed2004

A capillary zone electrophoresis (CZE) method for the determination of cyclizine hydrochloride in tablets and suppositories.

Current compendial methods of assay for the analysis of cyclizine tablets involve the use of UV spectrophotometry. Since this is a non-selective technique its application to more complex dosage forms, such as suppositories, is unlikely to be appropriate. There is therefore a need for the development of a highly specific quantitative analytical method, such as high performance liquid chromatography (HPLC) or capillary electrophoresis (CE). The latter technique was chosen in view of some specific advantages over HPLC, such as the use of relatively non-toxic aqueous buffers, as opposed to organic solvents, which obviates the use of expensive HPLC grade solvents making CE more cost effective. Cyclizine was analyzed in 50mM phosphate buffer (pH 2.3) and run at an applied voltage 25 kV. Detection sensitivity was enhanced by using a wavelength of 200 nm and samples were loaded hydrodynamically onto an uncoated fused-silica capillary (60 cm x 50 mm i.d.). Chlorcyclizine was used as the internal standard and resolution of both compounds was achieved in less than 7 min. Stress testing was undertaken in order to investigate the appearance of breakdown products. The method has the requisite accuracy, selectivity, sensitivity and precision to assay cyclizine in tablets and suppositories. Degradation products resulting from the stress studies did not interfere with the detection of cyclizine and the assay is thus stability-indicating.

Antiemetics↗
PubMed2003

A comparison of cyclizine, ondansetron and placebo as prophylaxis against postoperative nausea and vomiting in children.

Nausea and vomiting is a relevant and common problem with unfavourable sequelae in children undergoing some plastic surgery procedures. There is a lack of anti-emetic trials performed in children, with only a few investigating the roles of the older anti-emetic agents such as cyclizine compared with newer ones such as ondansetron. This randomised, controlled, double-blind study examined the effectiveness of a single dose of ondansetron (0.1 mg x kg-1), cyclizine (20 mg) and placebo (normal saline) in the prevention of postoperative nausea and vomiting in 150 children (mean age 3.6 years) undergoing plastic genitourinary procedures. Rates of previous postoperative nausea and vomiting and motion sickness were comparable across the groups. Postoperative vomiting was significantly reduced with ondansetron prophylaxis (p = 0.006) but there was no detectable anti-emetic effect with cyclizine. Furthermore, cyclizine caused pain on injection (p < 0.001).

Analgesics, Opioid↗
PubMed2006

A comparison of cyclizine and granisetron alone and in combination for the prevention of postoperative nausea and vomiting.

We conducted a randomised double-blinded study of 960 women undergoing day-case surgery to determine whether combination anti-emetic therapy of granisetron and cyclizine was more effective at decreasing the incidence of postoperative nausea and vomiting than these agents used alone. The women were randomly allocated to three groups to receive intravenous granisetron 1 mg, cyclizine 50 mg or both before induction of general anaesthesia. The incidence of postoperative nausea and vomiting was 77/322 (24%) in the granisetron group, 73/316 (23%) in the cyclizine group and 53/322 (17%) in those women given both drugs (p = 0.04). There was no difference in the requirement for rescue anti-emetic drugs. There were no differences in the anaesthetic techniques used in the three groups. We conclude that the risk of postoperative nausea and vomiting is less with cyclizine and granisetron given together than with either given alone.

Adult↗
PubMed1975

A comparison of the efficacy of cyclizine and perhenazine in reducing the emetic effects of morphine and pethidine.

1 The ability of cyclizine (50 mg) and perphenazine (2.5 and 5.0 mg) to counteract the emetic effects of pethidine (100 mg) and morphine (10 and 15 mg) was compared in women undergoing a standard minor operation with a standard anaesthetic. 2 Perphenazine (5.0 mg) was as effective an anti-emetic as cyclizine (50 mg) and both were more effective than perphenazine (2.5 mg). 3 The reduction in vomiting and nausea by cyclizine (50 mg) and perphenazine (5 mg) was approximately the same following pethidine (100 mg) and morphine (10 mg) but much less against the larger dose of morphine. 4 Both anti-emetics had a rapid onset of action but their anti-emetic activity did not last as long as the emetic effect of morphine. 5 Perphenazine (5 mg) was accompanied by an unacceptably high incidence of restlessness. 6 In clinical practice cyclizine (50 mg) is preferred to perphenazine (5 mg) as an anti-emetic.

Antiemetics↗
PubMed1988

Detrimental haemodynamic effects of cyclizine in heart failure.

The haemodynamic effects of intravenous cyclizine, an antiemetic that is widely given with opioids in left ventricular failure and myocardial infarction, were studied in 11 patients with severe heart failure. Cyclizine significantly increased systemic and pulmonary arterial pressures, and right and left ventricular filling pressures, and negated the venodilatory effects of diamorphine. The use of cyclizine in patients with heart failure should, therefore, be avoided.

Adult↗
PubMed1996

Cyclizine abuse by teenagers in Utah.

Substance abuse by teenagers is common, often involving use of alcohol and illicit drugs. Ingestion of cyclizine hydrochloride, a nonprescription medication, was noted to occur frequently in Utah for abuse reasons. A retrospective review was conducted of patients younger than 18 years of age over a 3-year period who intentionally ingested cyclizine identified from Utah Poison Control Center records. Eighty patients were included; 42 patients underwent hospital record review. Abuse accounted for 89% of cyclizine ingestions; hallucinations (70%) and confusion/disorientation (40%) were the most notable symptoms. Tachycardia (52%) and systolic hypertension (69%) were frequently present in patients who presented to a hospital. No serious complications occurred. This study illustrates teenage abuse of one nonprescription antihistamine presumably to induce hallucinations. Abuse of over-the-counter medications by adolescents may be more appealing than illicit drug use for numerous reasons, and may be more common than appreciated.

Adolescent↗
PubMed2003

Probable dystonic reaction after a single dose of cyclizine in a patient with a history of encephalitis.

A patient underwent an emergency Caesarean section under general anaesthesia for an antepartum haemorrhage. Following delivery of a live infant, cyclizine was administered in accordance with departmental anti-emetic protocol. On awakening she was confused, slow to articulate and had slurred speech. A computed tomography (CT) scan, which was performed to exclude an intracranial event, was normal. Her symptoms were suggestive of a lingual-facial-buccal dyskinesia as seen with dopamine antagonists. A presumptive diagnosis of a dystonic reaction to cyclizine was made. She received two doses of procyclidine before her symptoms completely resolved. Cyclizine has had a resurgence in popularity owing to the recent withdrawal of droperidol and anaesthetists should be aware that, although extremely rare, dystonic reactions may occur with this agent.

Acute Disease↗
PubMed1982

[The intoxication with cyclizin in infancy and adult age (Experiences of a contamination-information-central office) (author's transl)].

Epidemiological, clinical and therapeutic aspects obtained from 38 cases of intoxication with the antiemetic drug "cyclizine" in children and adults are discussed. The relative frequency of accidentally or purposely performed overdosage shows a decreasing tendency. The introduction of regulations after the prescription of cyclizine compounds, leaving a limited dose available without prescription and the introduction of a safety package to prohibit misuse by children are reported in their relationship with the epidemiologic data. A toxic dose of 5 mg/kg body weight, a minimal lethal dose (MLD) of about 80 mg/kg are evaluated and compared with previous published data. Differences of age in the development of the clinical picture of the cyclizine-intoxication with a disposition for the evolvement of convulsions in children compared to the total lack of convulsions in adults have to be pointed out. The management of overdoses follows general principles of treatment like gastric lavage, supporting care and includes the specific treatment with the antidote "physostigmin-salicylate", which causes a shortening of the time of recovery.

Adolescent↗