Cyclizine

266.38100

266.38

201-445-5

QRW9FCR9P2

756710|26608

DTXSID4022864

CRYSTALS FROM PETROLEUM ETHER|WHITE OR CREAMY WHITE CRYSTALLINE POWDER

R - Respiratory system

2933599090

6.48000

2.89920

Solid

0.9934 (rough estimate)

105.5-107.5 °C

150 °C @ Press: 0.09 Torr

1000 mg/L (at 25 °C)

PRACTICALLY ODORLESS

BETWEEN 7.6 & 8.6 (SATURATED SOLUTION)

166.7 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]|164.8 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

ODORLESS OR NEARLY SO & HAS BITTER TASTE; MELTS INDISTINCTLY & WITH DECOMP @ 285 °C /HYDROCHLORIDE/|PH (POTENTIOMETRICALLY DETERMINED, 1 IN 50 SOLN IN MIXT OF 2 VOL ALC & 3 VOL H2O) BETWEEN 4.5 & 5.5 /HYDROCHLORIDE/|PH BETWEEN 5 & 6 /LACTATE INJECTION/|WHITE, CRYSTALLINE POWDER OR SMALL COLORLESS CRYSTALS /HYDROCHLORIDE/|1 G IN ABOUT 115 ML H2O & 75 ML CHLOROFORM /HCL/

LIGHT-SENSITIVE

|Danger|H301 (97.44%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Despite widespread use, cyclizine and chlorcyclizine have rarely been linked to liver test abnormalities or to clinically apparent liver injury. In an isolated case report, cyclizine was linked to a case of clinically apparent liver injury in a child given the drug for several days to prevent motion sickness. The pattern of liver test abnormalities suggested mild viral hepatitis, but jaundice and symptoms recurred when cyclizine was restarted. There were no immunoallergic features and no evidence for autoimmunity. The reason for the general safety of cyclizine and chlorcyclizine may relate to low daily dose and limited duration of use.

COMBINATIONS OF CAFFEINE 100 MG WITH CYCLIZINE-HCL 50 & 100 MG DID NOT PRODUCE ANY SUBJECTIVE CHANGES OR CHANGES IN PERFORMANCE TESTS, DIFFERING FROM CONTROL.

For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo (dizziness caused by other medical problems).

Cyclizine and chlorcyclizine are first generation antihistamines that are used largely to treat or prevent motion sickness and nausea. Cyclizine has been linked to very rare instances of clinically apparent acute liver injury.

Antihistamines

Antiemetics; Histamine H1 Antagonists|ANTIHISTAMINE USED AS HYDROCHLORIDE & LACTATE IN PREVENTION & TREATMENT OF MOTION SICKNESS (NAUSEA, VOMITING & VERTIGO). IT IS ALSO PROBABLY EFFECTIVE FOR CONTROL OF POSTOPERATIVE NAUSEA & VOMITING.|DURATION OF ACTION IS ABOUT 4 HR.|...LARGE SCALE STUDY, INCL PREGNANT WOMEN RECEIVING CYCLIZINE DURING 1ST TRIMESTER, FAILED TO CONFIRM THAT DRUG HAD ANY TERATOGENIC EFFECT IN MAN WITH DOSES EMPLOYED.|For more Therapeutic Uses (Complete) data for CYCLIZINE (7 total), please visit the HSDB record page.

.../DO NOT/ EXCEED 4 TABLETS/DAY. /HYDROCHLORIDE/|.../IT/ SHOULD NOT BE USED IN WOMEN DURING PREGNANCY & THOSE LIKELY TO BECOME PREGNANT UNLESS SPECIFICALLY DIRECTED BY PHYSICIAN.|IN 1965 AN AD HOC COMMITTEE OF US FDA CONCLUDED THAT EVIDENCE OF TERATOGENIC EFFECTS IN HUMAN...WAS NOT SIGNIFICANT, BUT IT MADE NO SPECIFIC MENTION OF EYES.|...OFFSPRING OF PROBABLY SEVERAL THOUSAND WOMEN WHO HAD RECEIVED APPROX 150 MG CYCLIZINE/DAY DURING PREGNANCY...HAD A VARIETY OF NONOCULAR ABNORMALITIES, BUT STATISTICAL SIGNIFICANCE IN RELATION TO CYCLIZINE WAS UNCERTAIN.|For more Drug Warnings (Complete) data for CYCLIZINE (8 total), please visit the HSDB record page.

5. 5= EXTREMELY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 5-50 MG/KG; BETWEEN 7 DROPS & 1 TEASPOONFUL FOR 70 KG PERSON (150) LB.

Cyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)|Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)

BENZHYDROLPIPERAZINES & THEIR N-DEALKYLATION PRODUCTS ARE DISTRIBUTED IN ALL TISSUES OF RAT & ARE TRANSFERRED TO FETUS. /BENZYHYDROLPIPERAZINES/

Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine.|OXIDATIVE N-DEALKYLATION IS MAIN METABOLIC PATHWAY OF BENZHYDROLPIPERAZINES; CYCLIZINE.../IS/ TRANSFORMED INTO NORCYCLIZINE...|WITH A PURIFIED MIXED FUNCTION OXIDASE FROM LIVER MICROSOMES IN PRESENCE OF REDUCED PYRIDINE NUCLEOTIDE & O2.../CYCLIZINE IS/ OXIDIZED TO N-OXIDE.

20 hours

Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.|.../IT SEEMS/ THAT STIMULATION OF VESTIBULAR APPARATUS IS NECESSARY & SUFFICIENT...& THAT VESTIBULAR CEREBELLAR MIDBRAIN "INTEGRATIVE VOMITING CENTER" & MEDULLARY CHEMORECEPTIVE TRIGGER ZONE ARE...INVOLVED /IN MOTION SICKNESS/. IT IS...PROBABLE THAT EFFECTIVE ANTIHISTAMINES EXERT.../ACTION/ IN THESE CENTERS. /ANTIHISTAMINE/

LARGE DOSES MAY CAUSE DROWSINESS & DRYNESS OF MOUTH.|...MOST FREQUENT SIDE EFFECTS INVOLVE DIGESTIVE TRACT & INCL LOSS OF APPETITE, NAUSEA, VOMITING, EPIGASTRIC DISTRESS & CONSTIPATION OR DIARRHEA. ... ALLERGY MAY DEVELOP WHEN...GIVEN ORALLY, BUT MORE COMMONLY IT RESULTS FROM TOPICAL APPLICATION. ALLERGIC DERMATITIS IS NOT UNCOMMON. /H1 RECEPTOR BLOCKERS/|OTHER SIDE EFFECTS INCL DRYNESS OF MOUTH, THROAT, & RESP PASSAGES, SOMETIMES INDUCING COUGH; URINARY FREQUENCY & DYSURIA; PALPITATION; HYPOTENSION; HEADACHE; TIGHTNESS OF CHEST; & TINGLING, HEAVINESS, & WEAKNESS OF HANDS. ... GRAVE COMPLICATIONS SUCH AS LEUKOPENIA & AGRANULOCYTOSIS ARE VERY RARE. /H1 RECEPTOR BLOCKERS/|SIDE EFFECT WITH HIGHEST INCIDENCE, &...COMMON TO ALL DRUGS IN THIS GROUP, IS SEDATION. ... OTHER UNTOWARD REACTIONS REFERABLE TO CENTRAL ACTIONS INCL DIZZINESS, TINNITUS, LASSITUDE, INCOORDINATION, FATIGUE, BLURRED VISION, DIPLOPIA, EUPHORIA, NERVOUSNESS, INSOMNIA & TREMORS. /H1 RECEPTOR BLOCKERS/|For more Human Toxicity Excerpts (Complete) data for CYCLIZINE (10 total), please visit the HSDB record page.

Cyclizine

CYCLIZINE BASE IS REACTED WITH EQUIMOLAR QUANTITY OF LACTIC ACID. /LACTATE INJECTION/|MAREZINE [HYDROCHLORIDE] (BURROUGHS WELLCOME). ORAL: TABLETS 50 MG. RECTAL: SUPPOSITORIES 50 (PEDIATRIC) & 100 MG. /HYDROCHLORIDE/|MAREZINE [LACTATE] (BURROUGHS WELLCOME). INJECTION: SOLN 50 MG/ML IN 1 ML CONTAINERS. /LACTATE/|VALOID. /HYDROCHLORIDE/

AN ACID-DYE COMPLEX METHOD, USING BROMOCRESOL GREEN & BROMOPHENOL BLUE INDICATORS FOR ESTIMATION OF CYCLIZINE IN PHARMACEUTICAL PREPN IS REPORTED.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals