Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know...
-
Upload
melina-hines -
Category
Documents
-
view
237 -
download
2
Transcript of Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know...
![Page 1: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/1.jpg)
Ergot Alkaloids
Dr. Naila Abrar
![Page 2: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/2.jpg)
LEARNING OBJECTIVESLEARNING OBJECTIVES
After this session, you should be able to:• know the source and classification of ergot
alkaloids;• describe pharmacological actions of ergot
alkaloids;• comprehend the clinical indications of ergot
alkaloids; and• describe the adverse effects & contraindications
of ergot alkaloids.
![Page 3: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/3.jpg)
SOURCE:SOURCE: fungus - Claviceps purpurea
DISCOVERY:DISCOVERY:
ERGOTISM: ERGOTISM:
St. Anthony’s fire
![Page 4: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/4.jpg)
Claviceps purpurea
![Page 5: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/5.jpg)
CLASSIFICATIONCLASSIFICATIONAMINE ALKALOIDSAMINE ALKALOIDS6- Methylergoline, lysergic acid, lysergic acid
diethylamide, ergometrine (ergonovine), methysergide
PEPTIDE ALKALOIDSPEPTIDE ALKALOIDSErgotamine, dihydroergotamine, - ergocryptine, bromocriptine
![Page 6: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/6.jpg)
CHEMISTRYCHEMISTRY
• Ergoline nucleus• Derivatives of tetracyclic compound 6-methylergoline• Substituent in beta configuration at position 8 and a
double bond in ring D• Natural alkaloids: ergotamine, ergonovine
(derivatives of d-lysergic acid)• Semisynthetic & synthetic: dihydroergotamine,
bromocriptine, LSD, methysergide
![Page 7: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/7.jpg)
![Page 8: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/8.jpg)
PHARMACOKINETICSPHARMACOKINETICS
• Variable absorption from GIT• Ergotamine- poor oral BA• Speed of absorption and peak blood levels of
ergotamine improved with caffeine• Routes: oral S/L, I/M, I/V, nasal, rectal• Extensive metabolism• Ergonovine & methylergonovine - rapidly
absorbed
![Page 9: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/9.jpg)
MECHANISM OF ACTIONMECHANISM OF ACTION
• Multi-receptor function• Agonist, partial agonist, and antagonist at ,
serotonin • Presynaptic 5HT receptor (5HT1A/1D)
• Partial agonist at 5HT2 - uterus
• Partial agonist at CNS dopamine• Antagonist at blood vessels dopamine
![Page 10: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/10.jpg)
PHARMACOLOGICAL ACTIONSPHARMACOLOGICAL ACTIONS
CNS CNS • Hallucinogenic • LSD – drug abuse (agonist at 5HT2 in CNS)
• Nausea, vomiting – CTZ D2
• Decrease extrapyramidal symptoms - striatum D2
Inhibition of prolactin secretion – pituitary D2
Bromocriptine, pergolide, cabergoline
![Page 11: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/11.jpg)
VASCULAR SMOOTH MUSCLEVASCULAR SMOOTH MUSCLE• stimulation – VC – increase TPR & BP• Also vascular 5HT2
• Ergotamine- partial agonist• Vasospasm • Flow of blood to periphery decreases• Slow dissociation from receptors
![Page 12: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/12.jpg)
UTERUSUTERUS• Stimulation of & 5HT2
• More in uterus at term• Ergonovine (ergometrine) more selective • Rhythmic contractions and relaxation in
small doses and prolonged contracture at higher doses
![Page 13: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/13.jpg)
GITGIT• Stimulation of 5HT2 receptors
• Increase motility, diarrhea, abdominal cramps
• Dopamine receptors CTZ – anorexia, nausea, vomiting
![Page 14: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/14.jpg)
CLINICAL USESCLINICAL USESMIGRAINEMIGRAINETriptan drugsProdrome of attack – ergotamine tartrate Increase absorption with caffeineS/L 2 mg half hourly till relief - No more than 6mg
for each attack or no more than 10mg /wk0.25-0.5mg I/V or I/M total dose of 2 -3mg in 24hrs0.5 mg nasal spray- repeated after 15 mins if req.
total dose of 2 mg in 24hrs
![Page 15: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/15.jpg)
![Page 16: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/16.jpg)
HYPERPROLACTINEMIABromocriptine, cabergoline, pergolidePARKINSONISMBromocriptine, decrease EP effectsPOST PARTUM HEMORRHAGEErgonovine maleate 0.2 mg I/MDIAGNOSIS OF VARIANT ANGINAErgonovine to localize reactive segments of
coronaries during angiographySENILE CEREBRAL INSUFFICIENCYAlzheimer’s disease
![Page 17: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/17.jpg)
ADVERSE EFFECTSADVERSE EFFECTS
GIT:GIT: NVD, abdominal crampsVASOSPASM:VASOSPASM: Severe, gangreneCNS:CNS: Hallucinations, delirium, mania, drowsiness,
sedation, drugs of abuse - LSDRETROPERITONEAL FIBROSIS: RETROPERITONEAL FIBROSIS: MethysergideERYTHROMELALGIA:ERYTHROMELALGIA: with ergot derived
dopamine agonists like pergolide BP:BP: Raised UTERUS:UTERUS: Abortion
![Page 18: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/18.jpg)
Erythromelalgia
![Page 19: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/19.jpg)
CONTRAINDICATIONSCONTRAINDICATIONS
• Pregnancy• Renal disease• Hepatic disease• Psychotic illness• Collagen diseases• Peripheral Vascular disease
![Page 20: Ergot Alkaloids Dr. Naila Abrar. LEARNING OBJECTIVES After this session, you should be able to: know the source and classification of ergot alkaloids;](https://reader036.fdocuments.us/reader036/viewer/2022081503/5697bf711a28abf838c7df17/html5/thumbnails/20.jpg)