Transcript Active ingredient

Active ingredient:
Dry extract from Devil‘s claw root
Indications:
Rheumatism, arthrosis
Botany
Harpagophytum procumbens
(Burch.) De Candolle
Family:
Pedaliaceae
(sesame plants)
Synonyms:
Devil‘s claw
Wood Spider
Grapple plant
Origin:
Endemic in South and South-West
Africa (Namibia, Kalahari desert).
In sandy steppe regions, savannahs with
few trees or by waysides.
Botany
Medicinal drug:
Dried secondary tuber (Harpagophyti radix),
cut up into slices or pieces.
Brief profile

Enduring, weed-like plant.

Up to 1.5 m long sprouts, lying on the ground.

Water storage capacity of storage roots up to 90%.

Stalked leaves with deep lobes.

Flowers: bright violet-red in colour, funnel-shaped.

Widely branched system of primary and
secondary roots.

Secondary storage roots can develop several tubers with
a diameter of up to 6 cm.

Fruits: lignifying capsules with grapnel-like outgrowths
containing about 50 seeds.
Drug
Spectrum of ingredients: the same in both main and side roots
Concentration of ingredients: higher in the side roots
side roots are used for drug
preparation
Processing:
Crushing of the secondary storage roots (tubers of the side
roots)
Root fragments:
Colour:
yellowish grey or pale pink
Consistency: hard like horn
Taste:
bitter
Traditional medical use
Africa:
- indigestion
- blood diseases
- fever
- pains
- migraine
Europe: - metabolic diseases
- arthritis
- diseases in liver, gall-bladder, kidney and bladder
Further research towards the end of the 1950s gradually led
to Devil’s claw being applied mainly for treating rheumatic
diseases.
Phytochemistry

Extract from Devil's claw root: Mixture of substances
(just like any typical phytopharmaceutical)

Most important ingredients: Iridoid glycosides

Active component: Full extract
Ingredients

iridoid glycosides (1.1-3.6%): among others harpagoside
(at least 1.2%, very bitter), harpagide, procumbide

phenylethanol derivatives: verbascoside, isoacteoside

carbohydrates: among others stachyose, raffinose

flavonoids: kaempferol, luteolin

pharmacologically irrelevant are, among others, sterols,
alkanes, fats, waxes, gum resin, essential oils
Iridoid glycosides
Mechanism of action



Up to now, there are no consistent research results as to
the actual active ingredient(s) contained in the extract
from Devil's claw root.
Possibility of a dual action profile with an inhibition of the
cyclooxygenase or lipooxygenase way within the
arachidonic acid metabolism is being discussed.
Results of an in vitro study:
Devil's claw root extract contains additional substances
besides harpagoside that act to selectively inhibit the
lipooxygenase way and consequently the biosynthesis
of leukotrienes.
Mechanism of action


Harpagoside seems to contribute to the analgesic but
not the antiphlogistic effect
If rheumatism is considered to be a system disease
 another action approach via the
metabolism-regulating properties of
Devil's claw might be possible
Inflammation cascade
noxa
Cell membrane
Zellmembrane
phospholipids
Phospholipide
phospholipase
Phospholipase
arachidonic acid
lipooxygenase
Arachidonisäure
Lipooxygenase
leukotrienes
Leukotriene
immunocompetent
cells
(monocytes, T-cells)
immunokompetente Zelle
cytokines
(Monozyten, T-Zellen)
TNF-a, interleukins
Zytokine:
cyclooxygenase
Zyklooxygenase
prostaglandins
Prostaglandine
Toxicology
LD50 (Harpagophytum procumbens, full extract):
13.5 g/kg body weight p.o. (tests conducted on mice)
Tolerability
Side effects:
In rare cases nausea, diarrhea, vomiting, dizziness and
headache have been observed.
Hypersensitivity reactions (skin rashes, urticaria, facial
edema even including circulatory collapse (anaphylactic
shock) have been described very rarely. When suffering from
insulin-dependent diabetes mellitus, a blood-sugar increase
- which decreased after stopping the intake - has been
observed very rarely.
Contra-indications:
Patients suffering from gastric and duodenal ulcers (Devil‘s
claw root extract contains bitter substances that increase
gastric secretion).
Pharmacology
Devil's claw has become a scientifically excellently
researched and documented medicinal plant.
Tests demonstrated the analgesic, antiedematic and
antiphlogistic effects of the full extract.
These findings could be confirmed in practice by clinical
studies and physicians' empiric reports.
For the most part, the conducted studies revealed a distinct
antirheumatic potential.
Effects

antiphlogistic by COX- and
LOX-inhibition

analgetic

muscle-relaxing
Application for treating
rheumatic diseases

non-specific chronic backache (cervical
spine area, neck-shoulder-arm syndrome,
lumbar spine area, lumbago, ischialgia)

arthrosis (e.g. osteoarthrosis of the hip,
osteoarthrosis of the knee, degenerative
changes of the spine such as spondylosis,
spondylarthrosis)

active muscle hardening caused by unbalanced postures,
e.g. at computer workstations or due to athletic exertion
Application for treating
rheumatic diseases

chronic arthritis (primary chronic
polyarthritis, pcp)

non-articular rheumatism syndrome
(affecting musculature, ligaments and
tendons), e.g. fibromyalgia syndrome
Alternative to non-steroidal
anti-inflammatory drugs

Devil‘s claw has a similar principle of effect about the
COX-/LOX-inhibition (reduction of prostaglandins and
leukotrienes).

in contrast to the potential spectrum of side effects of the
NSAIDs, Cefatec® 480 is excellently tolerable.

No interaction in concentration or driving a car.

Onset of effect after few days to two weeks = in case of
intense, acute pains possibly overlapping start of therapy.
Proven therapeutic success with
Cefatec® 480 effervescent tablets
Multicentre practice study
Centres:
Indication:
Examination period:
Patient collective:
Medication:
196 practices
Degenerative disorders of the locomotor system
8 weeks
614 patients
(65.1 % of the patients were female and 34.0 %
male,average age of the patients 60.8 years)
The daily dosage was 2 effervescent tablets of
Cefatec® 480
 Especially suitable for a long-term treatment
 Reasonable alternative or accompanying therapy to nonsteroidal antirheumatic agents
Proven therapeutic success with
Cefatec® 480 effervescent tablets
Proven therapeutic success with
Cefatec® 480 effervescent tablets
Cefatec® 480 advantages at a glance

highly concentrated extract from
Devil‘s claw root for a gentle
therapy of inflammatory and
wear-caused diseases of the locomotor system

analgetic, antiphlogistic, muscle-relaxing

increases the flexibility of the joints

easy dosing and application
2 x 1 film coated tablet a day

good tolerability
Basic information
Fields of application
For supportive treatment of degenerative disorders of
the locomotor system.
Note: In acute conditions with reddening, swelling or
hyperthermia of joints and if complaints persist, a physician
should be consulted.
Composition
Active ingredient:
1 film coated tablet contains: Dry extract
from Devil's claw root (4.4 - 5.0:1) 480 mg. Extraction solvent: Ethanol 60 % (v/v).
Excipients:
Maize starch, microcrystalline cellulose, lactose monohydrate, colloidal anhydrous
silica, magnesium stearate, hypromellose, macrogol, talc, titanium dioxide E 171.
The quantity of carbohydrates taken in with a daily dose equals a white bread
exchange of 0.05.
Basic information
Contra-indications
This medicine may not be taken in cases of hypersensitivity to Devil's
claw or one of the excipients or in cases of gastric or duodenal ulcers. In case of
cholelithiasis, a physician should be consulted. There has not been sufficient
research for the use of this medicine during pregnancy and lactation. Therefore, it
should not be used during this period. Cefatec® 480 FT has not been researched
for children's use. Therefore, please refrain from giving Cefatec® 480 FT to
children under 12 years of age.
Warning
None known.
Dosage, kind and duration of application
Adults and children over 12 years take 1 film coated tablet twice daily.
The film coated tablets should be taken in the morning and the evening with the
meals with some liquid. Take Cefatec® 480 FT until you are free of pain.
Basic information
Side effects
In rare cases diarrhea, nausea, vomiting, dizziness and headache have been
observed. Hypersensitivity reactions (skin rashes, urticaria, facial edema even
including circulatory collapse (anaphylactic shock) have been described very
rarely. When suffering from insulin-dependent diabetes mellitus, a blood-sugar
increase - which decreased after stopping the intake - has been observed very
rarely.
Commercial forms
Film coated tablets: 20 pcs., 50 pcs.
Monograph
Devil’s Claw root, Harpagophyti radix
Official Monograph of the Bundesinstitut für Arzneimittel und Medizinprodukte (BfArM) (German Federal Institute for Drugs and Medical Devices)
Commission E (Phytotherapy), BAnz.-No. 43 dated March 02, 1989 (corr. BAnz.-No. 164, dated
September 01, 1990)
Name of Drug
Harpagophyti radix, devil’s claw root.
Composition of Drug
Devil’s Claw root consists of the dried, secondary tubers of Harpagophytum
procumbens (Burchell) de Candolle [Fam. Pedaliaceae], as well as their
preparations in effective dosage.
The drug contains bitter substances.
Uses
Loss of appetite, dyspepsia, supportive therapy of degenerative disorders of the
locomotor system.
Monograph
Contraindications
Gastric and duodenal ulcers. With gallstones, use only after
consultation with a physician.
Side Effects None known.
Interaction with Other Drugs None known.
Dosage
Unless otherwise prescribed: Daily dosage:
For loss of appetite: 1.5 g of drug; preparations of equivalent bitter value;
Otherwise: 4.5 g drug; equivalent preparations.
Mode of Administration
Comminuted drug for teas and other preparations for internal use.
Actions
Appetite-stimulating
Choleretic
Antiphlogistic
Mildly analgesic