analgesics i
TRANSCRIPT
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Presented by:Dr. Sugandha Sharma1st year PG
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Essentials of Medical Pharmacology- K.D.Tripathi (5th Ed.)
Pharmacology and therapeutics for dentistry- Neidle and Yagiela (3rd Ed.)
Pharmacotherapeutics in Dentistry-Gangarosa, Ciarlone, JeskePharmacology
- Dale,Rang and Ritter (4th Ed.)Basic & Clinical Pharmacology
- Bertran And Katzung
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PainAnalgesics-Definition
Classification
Routes of administrationOpioids-Classification
Opioid receptorsMechanism of action
Morphine-ActionsMorphine analgesiaPharmacological actions
PharmacokineticsAdverse effectsTherapeutic usesContraindications
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Codeine Fentanyl Tramadol PethidineMethadonePentazocineNaloxone
Strategies To Minimize Side EffectsUses in dentistryConclusion
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An unpleasant sensory emotional experienceassociated with actual or potential tissuedamage, or described in terms of suchdamage
I SP
Types of pain:A. Nociceptive (Tissue) Pain
B. Neuropathic (Nerve) Pain
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Definition:Analgesic is a drug that selectively relieves pain by acting inthe CNS or on peripheral pain mechanisms, withoutsignificantly altering consciousness.
ClassificationA. Opioid/Narcotic/Morphine like analgesics
B. Non opioid/Non narcotic/Nonsteroidal anti-inflammatory drugs.
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Oral Intramuscular Inj. Intravenous Inj.
PCA: patient controlledanalgesia
Epidural Administration Transdermal, Creams, gels and foam
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Opium Classification of Narcotic-Analgesics
1. Natural Opium Alkaloids
-Morphine-Codeine-Papaverine
2. Semisynthetic Opiates
-Heroin-Pholcodeine-Oxycodone
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3. Synthetic Opioids- Meperidine- Fentanyl- Methadone- Dextropropoxyphene- Tramadol
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CNS
Depressant effects:
(a) Analgesia Strong analgesic Relief of dull, poorly localized visceral pain
Nociceptive pain relieved better than neuretic pain Suppression of pain perception is selective.
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(b) Sedation
(c) Mood and Subjective effects
(d) Respiratory centre
(e) Cough centre
(f) Temperature regulating centre
(g) Vasomotor centre
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Stimulant effects:
(a) CTZ
(b) Edinger Westphal Nucleus
(c) Vagal centre
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CVS Causes Vasodilatation due to- Decreasing tone of blood vessels- Histamine release
GIT - Constipation.
NEUROENDOCRINE EFFECTS- Hypothalmic influence on pituitary is reduced.- Decreases levels of LH, FSH, ACTH whereasPROLACTIN & GH levels are increased.
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Smooth muscles- Biliary tract
- Urinary bladder
- Bronchi
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Oral absorption-Unreliable(High First pass Metabolism).Primarily metabolised in liver.
Freely crosses the placenta &can effect the foetus.
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1) Side Effects:Sedation, mental clouding, lethargyVomitingConstipationRespiratory depressionBlurring of visionUrinary retention
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2) Idiosyncrasy allergy
3) Apnoea- This may occur in new born when morphine is given tomother during labour.
-Treatment of choice Naloxone 10 ug /kginjected in the chord.
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4)Acute morphine poisoningIt is accidental ,suicidal or seen in drug abusers
Symptoms
Shallow & occasional breathing ,cyanosis ,pinpoint pupil ,fallin BP & shock .
Treatment
Respiratory support and maintenance of BPSpecific antidote Naloxone 0.4-0.8mg i.v
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5) Tolerance & dependenceHigh degree of tolerance if used repeatedly .
Withdrawal symptoms
Lacrimation ,sweating ,anxiety ,fear ,restlessness, tremor ,insomnia,
abdominal colic, diarrhoea.
Treatment Withdrawal of morphine &substitution with methadone
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Bronchial AsthmaInfants & ElderlyHead Injury
Undiagnosed AcuteAbdominal pain.Respiratory diseases(Emphysema, COPD)
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Equal analgesic efficacy to morphine
UNLIKE MORPHINE:- Less histamine release(Safer in ASTHMATICS)
- Less constipation
Used primarily as an analgesic (substitute of morphine)DOSE: 50-100 mg i.m, s.c/ orally(PETHIDINE HCL)100mg/ 2ml inj.;50-100mg Tab.)
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80 to 100 times more potent thanmorphine
Rapidly Onset of action (5 min)
Used for anesthesia and analgesia
DurogesicTransdermal patch (25-75g/hr)
Transdermal fentanyl(Durogesic)
Fentanyl lozenges(Actiq)
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Centrally Acting Analgesic.Has dual Norepinephrine & Serotonin reuptake inhibitoryeffects .10 times potent than morphine & produces less adverseeffects. Used in mild to medium intensity shortlasting pain.
DOSE: 50-100 mg oral/ i.v. 4-6 hrly(CONTRAMAL, DOMADOL)
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Mixed opioid agonist-antagonist action.Efficacy lower than morphine.Useful in Mild-Moderate pain conditions.Causes Tachycardia & rise in BP.Should not be used in opioid dependent subjects.
DOSE: 50-100 mg oral , 30-60 mg i.m /s.c(FORTWIN, FORTSTAR)
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No analgesic activity at all.Competitive antagonist at opioidreceptor & reverses all actions of morphine.Drug of choice for Morphine Poisoning.
Diagnosis of opioid dependence -it will precipitatewithdrawal reactions.
DOSE: 0.4 mg in 1 ml (NARCOTAN)
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Slow titration of doses.Changing the dosing regimen or route ofadministration.
Using a Nonopioid or Adjuvant Analgesic for anopioid sparing effect.Adding a drug to counteract the side effect.Constipation prophylaxis.
http://www.google.co.in/imgres?imgurl=http://www.toothachepainreliefsite.org/wp-content/uploads/2010/02/www.toothachepainrelieft.org_.jpg&imgrefurl=http://www.toothachepainreliefsite.org/&usg=__ywzDhk3wiusn_j8lJU3Dz50EX5U=&h=1024&w=1024&sz=160&hl=en&start=11&zoom=1&um=1&itbs=1&tbnid=ScoQujIeDHRmGM:&tbnh=150&tbnw=150&prev=/images?q=toothache+pain+relief&um=1&hl=en&tbs=isch:1 -
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Preanaesthetic medication
Postoperative pain
Fracture pain
Carcinoma
http://www.google.co.in/imgres?imgurl=http://www.toothachepainreliefsite.org/wp-content/uploads/2010/02/www.toothachepainrelieft.org_.jpg&imgrefurl=http://www.toothachepainreliefsite.org/&usg=__ywzDhk3wiusn_j8lJU3Dz50EX5U=&h=1024&w=1024&sz=160&hl=en&start=11&zoom=1&um=1&itbs=1&tbnid=ScoQujIeDHRmGM:&tbnh=150&tbnw=150&prev=/images?q=toothache+pain+relief&um=1&hl=en&tbs=isch:1 -
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