Valerian Valeriana officinalis L.

(Valerianaceae) Synonym(s) and related species

All-heal, Belgian valerian, Common valerian, Fragrant valerian, Garden valerian.
Many other Valerian species are used in different parts of the world.
Pharmacopoeias Powdered Valerian ( USP 32 ); Powdered Valerian Extract (
USP 32 ); Valerian ( BP 2009 , USP 32 ); Valerian Dry Aqueous Extract ( Ph
Eur 6.4 ); Valerian Dry Hydroalcoholic Extract ( BP 2009 , Ph Eur 6.4 );
Valerian Root ( Ph Eur 6.4 ); Valerian Tablets ( USP 32 ); Valerian Tincture (
BP 2009 , Ph Eur 6.4 ). Constituents Valerian root and rhizome contains a
large number of constituents which vary considerably according to the source of the
plant material and the method of processing and storage. Many are known to
contribute to the activity, and even those that are known to be unstable may produce
active decomposition products. The valepotriates include the valtrates, which are
active constituents, but decompose on storage to form other actives including
baldrinal, and volatile constituents. The volatile oil is composed of valerenic acids
and their esters, and other derivatives including isovaleric acid (which is responsible
for the odour of valerian), and others. Other constituents present include: the free
amino acids -aminobutyric acid (GABA); the flavonoids flavone 6-
methylapigenin, hesperidin and linarin; alkaloids of the pyridine type including
valerianine and valerine; and sterols including -sitosterol. Valerian dry
hydroalcoholic extract is an extract produced from valerian root and contains a
minimum of 0.25% sesquiterpenic acids, expressed as valerenic acid. Use and
indications Valerian is used particularly for stress and insomnia. It has long been
used as a hypnotic, sedative, anxiolytic, antispasmodic, carminative and
antihypertensive, and for hypochondriasis, migraine, cramp, intestinal colic,
rheumatic pains and dysmenorrhoea. Despite many pharmacological studies
showing sedative and anxiolytic effects, and binding or modulation of constituents to
GABA and other neuro- transmitter receptors, the clinical efficacy is not conclusively
proven. A recent study suggested that it is safe, but not necessarily effective;
however, many analytical reports also show that extracts and products of valerian
vary greatly in both chemical composition and biological activity, and it may be that
only certain preparations have any therapeutic benefit. Many commercial products
use valerian in combin- ation with hops, passiflora and other herbal extracts, and
there is some evidence that these may be more efficacious, although again this is not
clinically proven. The use of valerian as an aid to benzodiazepine withdrawal has
been suggested on the basis of GABA-receptor binding effects, and there is a small
study in mice which suggests that it may be useful to a limited extent; again this
has not been shown clinically. Pharmacokinetics An in vitro study using a
number of different valerian root preparations (capsules or tablets of the powdered
extract, and teas) found that the products tested inhibited the cytochrome P450
isoenzyme CYP3A4. 1 Other in vitro studies have found no effects, 2 or an
inductive effect at levels unlikely to be obtained clinically. 3 Generally, studies
suggest that any effect on CYP3A4 is unlikely to be of clinical importance, see
benzodiazepines, page 396. A further in vitro study 2 suggests that valerian
has no effect, or weak effects, on CYP1A2 (see also caffeine, page 397), CYP2C9 or
CYP2C19. This study also suggests that valerian does not affect CYP2D6, although
another in vitro study suggests that valerian may cause induction of CYP2D6,
but this was at concentrations that are unlikely to be attained in vivo . 3 These
effects are unlikely to be clinically relevant because a study in 12 healthy subjects
found that valerian root extract had no significant effects on the metabolism of
debrisoquine, a probe substrate for CYP2D6, 4 as did another clinical study using
dextromethorphan, page 397). A further clinical study suggests that valerian also
has no clinically relevant effect on CYP2E1, see chlorzoxazone, page 397. In vitro
investigations have suggested that valerian may inhibit P-glycoprotein, 1,5
although the authors of one study concluded that this is unlikely to be clinically
relevant, because the concentration at which this occurred is unlikely to be
attained in vivo , 5 and the findings of another study suggested that the
effects were much weaker than those of verapamil, a known, clinically relevant P-
glycoprotein inhibitor. 1 For information on the pharmacokinetics of individual
flavonoids present in valerian, see under flavonoids, page 186. Interactions
overview Valerian does not appear to affect the metabolism of alprazolam, caffeine,
chlorzoxazone, dextromethorphan or midazolam to a clinically relevant extent.
Valerian may increase the sleeping time in mice in response to alcohol and
barbiturates. Case reports describe possible interactions with ginkgo, see Ginkgo +
Herbal medicines; Valerian, page 214, V 394 and St John s wort and/or
loperamide, see St John s wort + Loperamide, page 373. For information on the
interactions of individual flavonoids present in valerian, see under flavonoids, page
186. 1. Lefebvre T, Foster BC, Drouin CE, Krantis A, Arnason JT, Livesey JF, Jordan SA.
In vitro activity of commercial valerian root extracts against human cytochrome
P450 3A4. J Pharm Pharm Sci (2004) 7, 265 73. 2. Zou L, Harkey MR,
Henderson GL. Effects of herbal components on cDNA-expressed cytochrome P450
enzyme catalytic activity. Life Sci (2002) 71, 1579 89. 3. Hellum BH, Hu Z,
Nilsen OG. The induction of CYP1A2, CYP2D6 and CYP3A4 by six trade herbal products
in cultured primary human hepatocytes. Basic Clin Pharmacol Toxicol (2007) 100,
23 30. 4. Gurley BJ, Gardner SF, Hubbard MA, Williams DK, Gentry WB, Khan IA,
Shah A. In vivo effects of goldenseal, kava kava, black cohosh, and valerian on
human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes. Clin Pharmacol
Ther (2005) 77, 415 26. 5. Hellum BH, Nilsen OG. In vitro inhibition of CYP3A4
metabolism and P-glycoprotein- mediated transport by trade herbal products. Basic
Clin Pharmacol Toxicol (2008) 102, 466 75