Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach

Table 1

A summary of physicochemical, pharmacokinetic and pharmacodynamic features of cinnarizine.

Properties	Pharmacokinetics	Pharmacodynamics
Piperazine derivative	Multiple dosing results in accumulation of drug	Antihistaminic, calcium channel blocker, antidopaminergic, anticholinergic and anti serotinergic.
Weak base	Rapid absorption through upper part of GIT ( = 2–4 h)	Selectively binds to calcium channels in open configuration specifically active in arteries
Poor aqueous solubility; (BCS class II)	Cross blood brain barrier by simple diffusion	Blocking effect on L-type calcium channels actively helpful for smooth muscle cells.
pH dependent solubility	Preferably metabolized in liver	Melanogenesis inhibition, regarded as skin whitening agents.
Highly lipophilic; ()	Metabolism by oxidation via cytochrome P450	Reduction in membrane permeability to extracellular calcium.
Melting point: 118–122°C	CYP2D6 and CYP2B6 selectively catalyze p-hydroxylation of cinnamyl phenyl ring and diphenyl methyl group respectively.	Exhibits inhibitory effect on potassium currents facilitating effect against vestibular vertigo.
UV ( = 253 nm)	Highly protein bound (91%).	Inhibitory action on 5HT serotonin uptake by platelets.
	Excretion is preferably via urine or in feaces to some extent.	Promote cerebral blood flow.
		Aggravates parkinsonism upon chronic medication.

References to the above mentioned points are cited in the text.