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[top]Introduction to Cyclizine



Cyclizine is an antihistamine piperazine derivative drug used as an anti-emetic which also exhibits strong anticholinergic effect. It is used to treat vertigo, motion sickness, nausea, vomiting and dizziness. It is often prescribed in conjunction with drugs that are known to cause nausea such as strong opiates like buprenorphine or dopamine agonists like Ropinirole or Pramipexole. It is also administered post-operatively to counteract nausea from general anaesthesia or opiates given for post-operative pain relief.

It is also used recreationally, most commonly as a potentiator for opiates. It works in a the same way to drugs such as diphenhydramine, meclozine and doxylamine although it is often preferred over most other antihistamines. Less commonly it is used and as a strong delirient causing extremely realistic hallucinations in the same way as plants containing tropane alkaloids such as atropine and scopolamine, including Datura and Belladonna.


[top]Using Cyclizine

[top]Ways of administration

Cyclizine's most common routes of administration are orally, intravenously and intramuscularly. It can also been injected subcutaneously. It must be in the right form to be injected, either sold as an injectable preparation or as pills that can be made into solution. Some pills gel up when added to water and cannot be injected. It can be combined with injectable opiates as a strong opiate booster in doses of 25-100mg or orally at 50-200mg.

Taken orally as a deliriant/hallucinogen much larger doses are needed however some users require relatively low doses to achieve visual effects. Some users need just 50-100mg to start to have visuals. The general consensus however is that doses of over 350mg is needed to give full visual effects with doses of 500-600mg producing full delirium. Intravenously it is around 4 times more potent.

It can also be insufflated having around double the potency of oral adminstation.

[top]Effects of Cyclizine


With opiates:
Increases euphoria
Strengthens 'nod' effects
Strong psychoactive effects such as visual and auditory hallucinations
Reduces nausea
Reduces itchiness
Increased rush when injecting

As a deliriant
Induces delirium
Visual and audio hallucination indistinguishable from reality
Euphoria
Amnesia
Doing things out of character
Dry mouth
Increased heart rate
Increased urination or sometimes difficulty urinating
Causes nausea at higher levels instead of reducing it
Random twitches and involuntary movement of limbs
Difficulty conversing
Slurred Speech
Jaw tension, 'gurning'
Sedation
Jumpiness, anxiety, fear

600mg oral dose:
Quote:
I was talking to my girlfriend, following her round the house and even annoying her, however she wasn't there. This was by far the most realistic of these types of true hallucinations I've had. She would talk to me and I would respond, then she would looked pissed off. I didn't dare ask if she was real or not just incase she was..........

........At some point I also put some of the cushions in the bin, why I have no idea.

Psychedelaholic.

[top]Combinations with Cyclizine


Alcohol - Increases the deliriant effects lowering the dosage required. Would be very dangerous if large amounts of alcohol were involved due to state of confusion and complete huge reduction in motor functions and reaction times.

Quote:
350mg Cyclizine + 6 shots of alchohol - This experience report is relatively innaccurate due to confusion and memory loss.

SWIM does however remember the feeling that he was incredibly heavy and found it very difficult to move. Also multiple hallucinations previously stated were present. In hindsight this was dangerous and irresponsible, i remember feeling psychologically effected from this experience due to terrifying hallucinations.

Fantasian.
Opiates - Strong potentiator favoured over most other antihistamines. Usually combined intravenously whereas other antihistamines cannot be injected. Used to be sold in conjunction with Dipipanone in a drug called Diconal but was discontinued due to high abuse potential. Is often combined with methadone, morphine, heroin and buprenorphine to simulataneously reduce nausea and itching and increase euphoria, sedation and create a psychedelic experience.

Contradictions:

Possible negative drug interactions
Potassium Chloride/Citrate (solid oral formulations) - Increased risk of upper gastrointestinal injury
Propoxythene (Darvon) - Could add to the CNS and respiratory depression effects
Sodium Oxybate (GHB) - Could add to the CNS and respiratory depression effects
Topiramate and Zonisamide (zonegram)- may potentiate the risk of oligohidrosis and hyperthermia particularly in pediatric patients

Possible disease interactions:
Asthma - may reduce the volume and cause thickening of bronchial secretions leading to increased obstruction of respiratory tract.
Cardiovascular - it can effect heart rate

[top]Different Uses for Cyclizine


As an anti-emetic:
Orally 25-100mg up to 3 times a day
I.V. 25-50mg up to 3 times a day


[top]Pharmacology of Cyclizine


It has a half like of 20hours and is metabolised by N-demethylation to the inactive molecule norcyclizine. Usually lasts 4-6hours when used medically.

Its anti-histamine action comes from antagonisation at the histamine H1-receptor, although it more like inverse agonism than antagonism. This means it binds to the site that an agonist would usually effectively reversing that receptors activity. Normal agonists do not bind to receptors but simply stop agonists binding as effectively. The antihistamine effects are usually used to treat symptons of allergic reaction such as runny nose, watery eyes, sneezing and itching.

Its anti-emetic effects are not actually fully understood. It is believed that is has an effect on the chemoreceptor trigger zone (CPZ) which is responsible for nausea. It is part of the Medulla which can induce vomitting in response to hormones such as histamine, dopamine and serotonin and blood-borne drugs like opiates. Cyclizine is also thought to directly work on the labyrinthine apparatus (Vestibular system) in the inner ear responsible for balance in most mammals.

Its deliriant and hallucinogenic effects are due to its central anticholinergic action. It blocks acetylcholine reaching the central (CNS) and peripheral nervous system.


[top]Chemistry of Cyclizine

Systematic (IUPAC) name:1-(diphenylmethyl)-4-methylpiperazine
Synonyms:N-benzhydryl-N'-methylpiperazine, N-methyl-N'-benzhydrylpiperazine, (N-benzhydryl)(N'-methyl)diethylenediamine, Compound 47-83, Wellcome preparation 47-83, Marzine, Marezine; Vaoloid (hydrochloride)
Molecular Formula:C18H22N2, C18H22N2.HCl (hydrochloride)
Molar mass: 266.39 g/mol, 302.85 g/mol (hydrochloride), 356.46 g/mol (lactate)
CAS Registry Number:82-92-8, 303-25-3 (hydrochloride)
Melting Point:105.5-107.5C
Boiling Point:no data
Flash Point:no data
Solubility:Freebase (25C) : <0.1mg/mL in water, 1.1 g/mL in chloroform, 0.17 g/mL in ether, 0.17 g/mL in ethanol. Hydrochloride : sparingly soluble in chloroform; slightly soluble in water, alcohol; insoluble in ether
Additionnal data:none
Notes:Freebase aspect : light sensitive crystals from petroleum ether. Hydrochloride aspect : white crystalline powder or colorless crystals; odorless, slightly bitter taste; protect from light
[1]


[top]The dangers of Cyclizine


The hallucinations both visually and auditory can be impossible to distinguish between reality essentially creating an awake dream state in which the dreams are superimposed onto whats real. This could put the user at danger or hurting themselves or others if they were to act upon what they saw. They could also get arrested or even sectioned as some users can forget they have even taken the drug so would not be able to explain their actions whilst still under the influence.


[top]Forms of Cyclizine

Solution for injecting - Cyclizine Lactate
I.V. preparations -
I.M. preparations - Marzine (50mg/ml)

Oral pills - Cyclizine Hydrochloride
50mg - Marezine, Emoquil (USA) and Valoid (UK), Nausicalm
25mg - Bonine (USA) for children


[top]Legal status of Cyclizine

[top]Brazil


Prescription only medication

[top]USA

Regulated but available over the counter

[top]Netherlands


Over the counter medication

[top]UK


Was available over the counter for many years but is now a prescription only medication

[top]Canada


Never available OTC and discontinued from prescription use in 1998


[top]History of Cyclizine



[top]Street names for Cyclizine



[top]The latest Cyclizine threads

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[top]References


[1]Merck Index, fifteenth edition (2013)


Created by psychedelaholic, 22-04-2011 at 10:57
Last edited by John_bob, 28-04-2014 at 20:31
Last comment by Docta on 02-08-2011 at 22:51
3 Comments, 34,389 Views

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