www.millenniumegypt.com
Transcription
www.millenniumegypt.com
6-7-8 www.millenniumegypt.com Some uses and actions of some medicinal barks Antimalarial, anti-arrhythmic Cinchona Hemostatic (rectal, nasal bleeding) Hamamelis Tonic, stomchic Cinchona + Cascarilla Antispasmodic Cassia, Cinnamon, Canella Laxative Cascara, Frangula Astringent Hamamelis, Pomegranate Antipyretic, analgesic, antiinflammatory Salix Anthelmintic Pomegranate Respiratory disorders Wild cherry, Cascarilla Page | 1 Classification of barks according to active constituents Alkaloids Cinchona Pomegranate Tannins Hamamelis Pomegranate Cinchona Volatile oil Cinnamon Cassia Canella Cascarilla Glycosides Cyanogenic Wild Cherry Saponin Quillaia Anthraquinones Cascara Frangula Phenolic Salix Page | 2 Barks containing alkaloids: (Associated with tannins) Items Syn. Action & Uses & Pharmaceutical preparation Active constituents Origin Pomegranate bark قشر الرمان Cinchona bark قشر الكينا Barks containing tannins Witch-Hazel Bark قشر هماميلس Quishrul kiena, Countess bark Quishrul Rouman Hamamelis Dried stem & root barks of Cinchona succirubra (red cinchona) C. Ledgeriana & C. calisaya (yellow cinchona) C. officinalis (pale cinchona) Fam. Rubiaceae. 1. About 30 alkaloids (5-15%): Quinine, Quinidine, Cinchonine, Cinchonidine [present in comination with Quinic acid]. Dried stem & root barks of Punica granatum Fam. Punicaceae Dried stem bark of Hamamelis virginiana Fam. Hamamelidaceae 1. Alkaloids: a) Four liquid alkaloid: Hamamelitannin (GALLOTANNIN 7%) and smaller amounts of condensed tannins. 2. Tannins known as Cinchotannic acids (CATECHOL tannins) (Alkaloids combined with tannin.) 1. Bitter tonic and stomachic (due to Quinine) Tincture Cinchona (liquid extract); take 20 drops in plenty of water before meals. 2. Hair tonic & stimulates hair growth (due to Quinine) Tonoscalpine lotion (contain Quinine HCl inc. blood flow) 3. Antimalarial (due to Quinine & Quinidine) Quinate Tablets 4. Anti-arrhythmic for atrial fibrillation ( االرتجاف األذينيdue to Quinidine) Cardioquin 5. Antirheumatic (due to Cinchonine & Cinchonidine) 6. A decoction and infusion are used for sore throat as gargles (due to tannins) boil Decoction: pd. + water → boil Infusion: water → +pd Pelletierine (punicine) Isopelletierine, Methyl-pelletierine Methyl-isopelletierine b) One crystalline alkaloid: Pseudo-pelletierine 2. Tannins (22%): PYROGALLOL tannins 1. Anthelmintic: for tapeworms (in small intestine – 15m) [due to alkaloids] 2. Astringent: in diarrhea (due to tannins) N.B. - Ascaris (lives in small intestine) anthelmintic used: santonica flower (oral dose) - Tapeworms (lives in small intestine) anthelmintic used: pomegranate bark (oral dose) - Thread worms (lives in large intestine) anthelmintic used: quassia wood (enema )حقنة شرجية 1. Astringent for diarrhea. 2. Haemostatic in excessive menstruation, haemorrhoids, rectal and nasal bleeding. Avenoc ointment (for haemorrhoids) 3. Anti-inflammatory for prostate congestion. Decongestyle suppository (congestion & inflammation of the prostate) 4. In eye and skin inflammation. 5. Anti-aging or anti-wrinkle in skin preparations (skin toner) مطبوخ منقوع Page | 3 Contraindications 1. In pregnancy (as quinine cause bleeding then abortion) 2. Iron deficiency anemia (due to tannins) 3. Hypersensitivity to cinchona alkaloids Drug interaction: Potentiation of concurrently administrated anticoagulants (as Warfarin, Heparin) leading to bleeding. 1. Test for Cinchona red (Dry heat test): ∆ 𝑖𝑛 𝑑𝑟𝑦 𝑡𝑒𝑠𝑡 𝑡𝑢𝑏𝑒 Pd → purplish red vapours → condensed as 𝑎𝑙𝑐𝑜ℎ𝑜𝑙 (50%) purplish-red tarry drops → blue fluorescence Tannins are contraindicated in: - Constipation - Iron deficiency anemia - Malnutrition Test for tannins: 𝑠ℎ𝑎𝑘𝑒,𝑓𝑖𝑙𝑡𝑒𝑟 Pd + water → ppt. Test for tannins: + . 𝐹𝑒𝐶𝑙3 → bluish- black 𝐹𝑒𝐶𝑙3 Pd + water → filtrate → bluish-black ppt. Remember: Test for identity 2. Test for alkaloids (Mayer’s test): 𝑠ℎ𝑎𝑘𝑒,𝑓𝑖𝑙𝑡𝑒𝑟 Pd + dil. HCl → Mayer’s reagent → a creamy ppt. Mayer’s test is a general test for alkaloids. Catechol tannins (=condensed tannins) gives Greenish black color with 𝐹𝑒𝐶𝑙3 . 3. Test for quinine and quinidine: 𝑏𝑜𝑖𝑙,𝑓𝑖𝑙𝑡𝑒𝑟 Pd. + dil. 𝐻2 𝑆𝑂4 → Other items + water → blue fluorescence Cinchonism (quinism): - Is a pathological condition caused by an overdose of quinine, quinidine or cinchona bark. - Mild cinchonism (standard therapeutic doses): includes ringing طنينof ears, blurred vision, abdominal pain, nausea, vomiting and diarrhea. - Sever cinchonism (large doses): skin rashes, deafness, blindness (damage of auditory and optic nerves), death. - Most symptoms of mild cinchonism are reversible and disappear once the drug is withdrawn. Pyrogallol tannins (=gallotannins, hydrolysable tannins) gives Bluish black color with 𝐹𝑒𝐶𝑙3. Test for purity: Pomegranate bark contains no phloem fibers. Stem bark Root bark 1. Curved, channeled 1. Recurved, flat 2. Lenticels, lichens 2. No lenticels; no present lichens 3. 0.5 % alkaloids ↓ 3. 0.6 % alkaloids ↑ Page | 4 Treatment of overdose (severe cinchonism): If ingestion is recent, perform the following: 1. Gasrtic lavage or emesis induction. 2. Administration of activated charcoal (to reduce absorption of any remaining drug) 3. Administration of a hypertonic cathartic (sodium sulfate in water) [to hasten passage of unabsorbed drug through GIT] Morphological differences bet. Stem & root barks: Stem bark Root bark 1. Epiphytes 1. No epiphytes 2. Single, double quill 2. Curved, channeled 3. Laticiferous tube 3. No laticiferous tube 4. Normal fibers 4. Forked fibers 5. No sclereids 5. Sclereids 6. Lower % of alkaloids 6. Higher % of alkaloids N.B: Pomegranate & canella barks contain no phloem fibers. ∴ their powders don’t show any phloem fibers under microscope Questions: 1. Explain: The absence of laticiferous tube in root bark?? Or the absence of 1ry cortex?? Or the whole cortical part of the root bark consists of phelloderm (2ry cortex)?? Ans: In root bark, phellogen is formed in the pericycle, ∴ all outer tissues including 1ry cortex (showing laticiferous tubes) changes to rhytidoma. The whole cortical part of the bark consists of phelloderm (2ry cortex). 2. Give reason: The use of castor oil or saline with pomegranate bark. Ans: - Pomegranate only paralyze worms but not expel them. - Castor oil or saline act as purgative so used with pomegranate bark to expel the paralyzed worms. Page | 5 Barks containing volatile oil Action & Uses constituents Items Syn. Origin Cinnamon bark قشر دار صيني Ceylon Cinnamon, Darsieni, Quirfa Helwa Dried decorticated bark of shoots of coppiced trees of Cinnamomum zeylancium Fam. Lauraceae Cassia bark قشر قرفة صيني Chinese cinnamon Dried bark of Cinnamomum cassia Fam. Lauraceae Canella bark قشر قرفة بيضاء White Cinnamon, Wild cinnamon Dried decorticated bark of Canella alba Fam. Canellaceae. - Occurs in channeled pieces or N.B. Coppicing: single quills. Is a method in which tree stems are repeatedly cut down to near the ground level. 1. Cut close to base in winter 2. Following spring shoots rapidly regrow from stool. 3. 7-20 years later coppice ready for harvest 1. Volatile oil composed of cinnamic 1. Volatile oil containing mainly aldehyde (55-65%) and eugenol (4-8%) cinnamaldehyde (85%), no 2. Condensed tannins (1%) eugenol. 3. Mucilage (pectose and callose) 2. Condensed tannins (10%) 3. Mucilage (pectose) Secretory str. → oil cell 1. Antispasmodic in GIT disorders, carminative in flatulence. 2. Sedative and analgesic (Cinnamaldehyde) 3. Antiseptic and mild astringent, flavouring agent. 4. Emmenagogue, stimulates the uterus and encourage menstrual bleeding. 5. Helps maintain normal blood sugar (Cinnamaldehyde) Cascarilla bark قشر العنبر Sweet wood bark, Quishrul Anbar Dried stem bark of Croton eleuteria Fam. Euphorbiaceae - Allied drug for cinnamon. Occurs in quills or curved pieces. Decorticated by removing the cork. First layer is sclerenchymatous phelloderm (2ry cortex). - No phloem fibers. 1. Volatile oil: (0.5-1.28%) Eugenol, cineole, caryophylline and canellal (antifungal sesquiterpene dialdehyde). 2. Resin & mucilage. 3. No tannins 1. Volatile oil (1-1.5%): Eugenol, limonene, vanillin. 2. Bitter principle, cascarillin. 3. Alkaloid cascarilline. 1. Carminative and has anti1. Improve poor digestion. 1. ulcer properties. 2. Aromatic stimulant and tonic. 2. Sedative and analgesic (has a 3. Antifungal (due to canellal). 2. soothing effect) in 3. abdominal pain. N.B: Cassia and Canella are allied 3. Flavouring agent. drugs of Cinnamon. 4. 4. Used as a substitute for Remember: Mucilages are classified into: cinnamon. R𝐮𝐭𝐡𝐞𝐧𝐢𝐮𝐦 𝐫𝐞𝐝 1. Pectose type ⇒ 𝐂𝐨𝐫𝐚𝐥𝐥𝐢𝐧 𝐬𝐨𝐝𝐚 2. Callose type ⇒ 3. Neutral type ⇒ red color red color 𝐌𝐞𝐭𝐡𝐲𝐥𝐞𝐧𝐞 𝐛𝐥𝐮𝐞 Bitter stomachic: often mixed with rhubarb. Expectorant in chronic bronchitis. Fragrant component in soaps, creams & lotion. In fumigating mixtures. Blue color Page | 6 Drug interaction: - Cinnamon may increase the risk of bleeding when taken with drugs that increase the risk of bleeding, as aspirin, anticoagulants. - N.B: Cinnamaldehyde inhibits the aggregation of plates and may reduce the tendency of blood to clot i.e. has anticoagulant effect. - Cinnamon may lower blood sugar levels. Caution when using antidiabetic medications. Other items Contraindication: Not recommended during pregnancy and lactation. - Description: Pleasant aromatic odour. Bitter taste. When burned it gives an agreeable fumigating odour. Inner surface shows remains of wood. ∴ the bark named sweet wood bark. Outer layer shows a white or greyishwhite cork with: 1. Chalky appearance due to presence of numerous Ca.OX prisms in inner walls of cork cells. 2. Chequred appearance due to longitudinal wrinkles and transverse furrows. Pharmaceutical preparation: Carminex (syrup) - Composition: Each 100ml contains: Cinnamon oil 0.1 ml Fennel oil 0.1 ml Caraway oil 0.1 ml - Indications: - Flatulence - Digestive disorders, spasm, colic, nausea … Page | 7 Main differences between Cinnamon and Cassia: Items Origin Shape Color Kind Taste Microscopically Cinnamon Cassia Dried decorticated bark of shoots of coppiced trees of Cinnamomum zeylancium Fam. Lauraceae Single or double compound quills Yellowish-brown Decorticated Sweet, less astringent Cork No cork Pericycle Continuous Keratenchyma Present Elements diameter Less than 30 μ of fiber Diameter of starch Less than 10 μ Dried stem bark of Cinnamomum cassia Fam. Lauraceae Channeled or single quills Dark brown Complete bark Sweet more astringent Presence of cork Discontinuous Absent More than 20 μ More than 10 μ Active constituents Chemical tests Volatile oil (0.5-1%): Volatile oil (1-1.5%): Cinnamic aldehyde (55-65%) Cinnamic aldehyde (85%) Eugenol (4-8%) No eugenol Tannins (1%) More tannins Mucilage More mucilage Sudan III + ve + ve For V.O For FeCl3 Blue color - ve eugenol KOH Needle crystals - ve For mucilage Ruthenium red Corallin soda + ve (pectose) + ve + ve (callose) - ve Page | 8 Barks containing glycosides Items Syn. Origin a) Barks containing cyanogenic glycosides b) Barks containing Saponin glycosides Wild Cherry bark قشر كرز بري Quillaia bark قشر الكوياليا Dried stem bark of Prunus serotina Fam. Rosaceae. - Collected in the autumn, at which time it is most active. - Carefully dried and kept in air-tight container. - Odour: odourless, but when slightly moist it has an odour of benzaldehyde (bitter almond). The cyanogenic glycoside: prunasin. 𝑃𝑟𝑢𝑛𝑎𝑠𝑒 𝑒𝑛𝑧.𝑖𝑛 𝑏𝑎𝑟𝑘/𝑚𝑜𝑖𝑠𝑡𝑢𝑟𝑒 Prunasin → HCN + benzaldehyde + dextrose. (bitter almond odour). Antitussive (cough sedative); for chronic, dry & whooping coughs and in bronchitis. (antibacterial, antiviral & mild sedative actions). Action & Uses constitue nts Test for identity Test for cyanogenic glycoside: (Guignard’s test): Put small pieces of bark + 𝐻2 𝑂 in a test tube closed with cork holding a strip of moistened sodium picrate paper (Guignard reagent) between it & the tube, HCN evolved will change the yellow color to a brick-red color. Soap bark, Panama wood Dried inner bark (decorticated) of Quillaia saponaria Fam. Rosaceae. - Outer surface is: Longitudinally striated, streaked with reddish brown color where rhytidoma is imperfectly removed. - Bark consists entirely of: phloem tissues (inner bark). - Characterized by styloid prisms. Saponin glycosides: - quillajic acid - quillaia sapotoxin Only for external use: 1. Used as a hair tonic and anti-dandruff in hair shampoos. 2. Used as a cutaneous stimulant منشط للجلدin the treatment of skin ulcers and eruptions (rashes) طفح جلدي 3. Foaming agent in fire extinguishers. Caution: Must not used as: 1. Oral administration: as when taken by mouth produce severe GIT irritation. 2. Intravenous injections The injection of large amounts may result in systemic poisoning with liver damage, respiratory failure, convolutions and coma as saponins cause haemolysis of RBCs. 1. Froth test (foaming test): Shake pd. with water → persistent froth. 2. Haemolysis test: aqueous extract of pd produce haemolysis of RBCs. Page | 9 Barks containing glycosides c) Barks containing anthraquinone glycosides Items Syn. Origin Action & Uses constitue nts Cascara bark )قشرة مقدس (الكسكرة Cascara sagrada, Cascara Buckthorn Dried stem bark of Rhamnus purshiana Fam. Rhamnacea. - Collected at least one year before being employed medicinally. Anthraquinones: Cascarosides A, B, C, D 1. Laxative or purgative in large doses (fecal softener) - Occasional constipation - Disorders that aquires easy evaculation with soft stool as: anal fissures, hemorrhoids, after recto-anal operations. 2. Tonic and stomachic in small doses. 3. Cascara: Cathartic with disagreeable taste, Frangula: Agreeable cathartic, preferable than cascara (less disagreeable taste) 1. Borntrager’s test: 𝑏𝑜𝑖𝑙 Pd + alc. KOH → Chemical test Frangula bark قشر العوسج األسود Quishrel Awsagel-Aswad Dried stem bark of Rhamnus frangula Fam. Rhamnaceae. - Collected at least one year before employed medicinally. Anthraquinones: Frangulins A, B 𝑎𝑚𝑚𝑜𝑛𝑖𝑎 → 𝐻𝐶𝑙 𝑆ℎ𝑎𝑘𝑒 𝑤𝑖𝑡ℎ 𝑒𝑡ℎ𝑒𝑟 filtrate → cold solution → d) Barks containing Phenolic glycosides Willow bark قشر الصفصاف Salix Dried barks of Salix alba, Salix purpurea and other species of Salix. Fam. Salicacea. - Phenolic glycosides (1.5-11%), salicin (salicylic derivatives) P-coumaric, caffeic and ferulic acids, salicyl alcohol (saligenin) Tannins (8-20%) Antipyretic, analgesic, anti-inflammatory, astringent actions. Indicated in: Feverish colds and infections (influenza) Rheumatic disorders, gout Mild headache Diarrhea (tannin) ethereal layer orange red color in aqueous layer 2. Microsublimation test: 𝑎𝑙𝑘𝑎𝑙𝑖 heat pd. in dry tube → yellow crystal → Reddish-brown color 3. Test for callose mucilage: T.S. + corallin soda, the callus plates acquire a red stain. → +ve in cascara / –ve in frangula Page | 10 Side effects Pharm. Prep. Other items - Cramp or gripping of GIT. - Repeated defecation → hypokalemia (low conc. of potassium 𝐾 + in the blood) leading to cardiac disorders, muscular weakness. (Long-term use: disturbance of electrolyte balance especially potassium deficiency) - Mucinum tablets: cascara extract - Normacol: 8% frangula - Normalin tablets: Non-griping laxative (cascara extract 70mg + hyoscyamus 10 mg) Mechanism of action: Stimulant or irritant laxatives (cascara, frangula) increase the peristaltic movement of the intestine. - Possibility of gastrointestinal troubles (due to tannins) - Possibility of urticaria, asthma and bronchial spasms (with known hypersensitivity to salicylates). Contra indications: - In intestinal obstruction and inflammation. - During pregnancy and lactation. Colitis. - Children under 12 years old. Salicylic acid inhibits the synthesis of prostaglandins and leukotrienes via cyclo-oxygenase and lipo-oxygenase enzymes. The analgesic action of willow is slow-acting but last longer than standard aspirin products. Willow bark is the precursor of acetylsalicylic acid (aspirin). Mechanism of action: 𝑠𝑝𝑙𝑖𝑡𝑠 𝑏𝑦 𝑡ℎ𝑒 𝑖𝑛𝑡𝑒𝑠𝑡𝑖𝑛𝑎𝑙 𝑓𝑙𝑜𝑟𝑎 Salicin → salicylic acid 𝑎𝑏𝑠𝑜𝑟𝑏𝑒𝑑,𝑜𝑥𝑖𝑑.𝑖𝑛 𝑏𝑙𝑜𝑜𝑑 & 𝑙𝑖𝑣𝑒𝑟 saligenin + glucose→ Powdered willow is characterized by: - Crystal sheath containing prisms of CaOX. - Scattered large cluster crystals of Ca.OX. Page | 11 Questions: 1. Give reason: cascara and frangula must be stored at least one year before use? Ans: Fresh bark contains: Anthanols, anthrones (active cathartic but emetic, irritant) Stored bark contains: corresponding anthraquinones (less emetic, less irritant, mild cathartic) changes in intestine to anthranols. After 1 year storage: The irritant principles (anthranols) present in freash barks changes to less irritant corresponding anthraquinones. Anthranols Irritant cathartic (Fresh bark) 𝑜𝑥𝑖𝑑𝑎𝑡𝑖𝑜𝑛 → anthraquinones 𝑖𝑛𝑡𝑒𝑠𝑡𝑖𝑛𝑒 ← Less irritant, mild cathartic (after 1 year storage) 2. Explain: 1) Role of hyoscyamus in normalin tablets. Hyoscymus acts as antispasmodic that treats the gripping effect of cascara. 2) Normalin tablets is contraindicated in patient with cardiac disorders. As Normalin contains cascara which on long-term use causes repeated defecation and finally leads to hypokaleimia. 3) Use of Mucinum tablets after recto-anal operations, haemorrhoids. Bec it soften the stool. Page | 12