 Central Nervous System Stimulation
-primary action of a diverse group of
pharmacological agents -adverse effect
associat...
INDIAN DENTAL ACADEMY
Leader in continuing dental education
www.indiandentalacademy.com

www.indiandentalacadmey.com
 Behavioral Manifestations of CNS
Stimulation
 mild elevation in alertness, decrease in
drowsiness and lessening of fati...
Molecular Basis of CNS
Stimulation
Imbalance between inhibitory and excitatory
processes as in the brain. This hyper-excit...
Classification of CNS
Stimulants
 Analeptic Stimulants



Respiratory Stimulants
Convulsants

 Psychomotor Stimulant
...
Analeptic Stimulants
diverse chemical class of agents
majority can be absorbed orally
have a short duration of action - pr...
 Doxapram and Nikithamide - used to
counteract postanesthetic respiratory depression
and for acute hypercapnia in chronic...
 Strychnine is a source of accidental poisoning.
Also used to study CNS mechanism because of
its relatively specific acti...
www.indiandentalacadmey.com
Treatment of Strychnine
Poisoning
(1) Remove/reduce external sensory stimuli
(2) Diazepam or Clonazepam I.V. or nitrous
ox...
PSYCHOMOTOR
STIMULANTS
 Drugs of Primary Importance
Amphetamine - prototype
Methamphetamine
Methylphenidate

www.indiande...
CHARACTERISTICS
 all compounds are absorbed well orally
 large portion of untransformed amphetamine is
excreted unchange...
Pharmacological Actions
 The primary effects of an oral dose are
wakefulness, alertness, decrease fatigue;
mood elevation...
 Stimulate the respiratory center, especially when
respiration is depressed by centrally acting drugs,
(barbiturates and ...
Mechanisms of Action
 Releases monoamines at synapses in
the brain and spinal cord.
 Inhibits neuronal uptake of monoami...
Therapeutic Uses
 Hyperkinesias - Methylphenidate
 Narcolepsy - Amphetamine or
methylphenidate
 Obesity - Fenfluramine
...
Adverse Effects
 CNS: Euphoria, dizziness, tremor, irritability,
insomnia, Convulsion (at higher doses),
hyperthermia and...
 Drug Interactions:




Tricyclic antidepressant
Antihypertensive Agents
Foods high in tyramine content

www.indianden...
METHYLXANTINES
 Caffeine:




Coffee (100-150 mg/cup)
Tea (30-40 mg/cups)
Cocoa (15-18mg/cup)

 Theophylline: Tea and...
Mechanisms of Action
 Increase cyclic nucleotide concentration
 Blocks adenosine receptors
 Alters intracellular calciu...
 Caffeine, the most widely used drug in
the world, is a stimulant. Commonly
found in coffee, tea, soft drinks,
chocolate ...
Pharmacological Activity/
Adverse Effects
 Low Doses: 50-250mg/Caffeine (Oral Doses)
Increase mental alertness, decrease
...
 Cardiovascular System: Increase rate
and force of the heart by directly
stimulating myocardium (low doses)
Tachycardia a...
 Smooth Muscles: Relaxes vascular
smooth muscle (Theophylline »Caffeine)
 Kidney: All xanthines are capable of
producing...
Adverse effects
 Stimulate gastric secretions in patients
with ulcer
 Dehydration in children due to vomiting
and transi...
Therapeutic Uses
 Caffeine + plus ergot alkaloid
(Ergotamine): used to treat migraine
headaches
 OTC preparations: Theop...
NICOTINE
 CNS Effects:
 Powerful CNS stimulant at lower doses;
Large doses produce clonic convulsion, then
depress CNS, ...
 Cardiovascular Effects
Tachycardia
Increased blood pressure
Pupillary constriction
Cardiovascular collapse - due to CNS
...
COCAINE
 Psychomotor stimulant
 local anesthetic
 Chemistry- alkaloid from coca plant
alkaloid is highly lipid-soluble
...
Routes of Administration
 Chewing: with an-alkaloid material (South
America)
 Sniffing: hydrochloride salt -absorption: ...
Pharmacokinetics
large vol. of distribution
quickly metabolized: half-life 30-90 minutes
principal metabolites: a) Ecogoni...
www.indiandentalacadmey.com
www.indiandentalacademy.com
Leader in continuing dental education

www.indiandentalacadmey.com
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Central nervous system stimulants /certified fixed orthodontic courses by Indian dental academy

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The Indian Dental Academy is the Leader in continuing dental education , training dentists in all aspects of dentistry and offering a wide range of dental certified courses in different formats.

Indian dental academy provides dental crown & Bridge,rotary endodontics,fixed orthodontics,
Dental implants courses.for details pls visit www.indiandentalacademy.com ,or call
0091-9248678078

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Central nervous system stimulants /certified fixed orthodontic courses by Indian dental academy

  1. 1.  Central Nervous System Stimulation -primary action of a diverse group of pharmacological agents -adverse effect associated with many drugs www.indiandentalacadmey.com
  2. 2. INDIAN DENTAL ACADEMY Leader in continuing dental education www.indiandentalacademy.com www.indiandentalacadmey.com
  3. 3.  Behavioral Manifestations of CNS Stimulation  mild elevation in alertness, decrease in drowsiness and lessening of fatigue (Analeptic Effect)  increased nervousness and anxiety -convulsions. www.indiandentalacadmey.com
  4. 4. Molecular Basis of CNS Stimulation Imbalance between inhibitory and excitatory processes as in the brain. This hyper-excitability of neurons results from:  potentiation or enhancement of excitatory neurotransmission(e.g. amphetamine)  depression or antagonism of inhibitory transmission (e.g. Strychnine)  presynaptic control of neurotransmitter release (e.g. picrotoxin) www.indiandentalacadmey.com
  5. 5. Classification of CNS Stimulants  Analeptic Stimulants   Respiratory Stimulants Convulsants  Psychomotor Stimulant  Sympathomimetics or Adrenergic CNS Stimulants  Methylxanthines www.indiandentalacadmey.com
  6. 6. Analeptic Stimulants diverse chemical class of agents majority can be absorbed orally have a short duration of action - primary expression of pharmacological effect is convulsions (tonic-clonic) uncoordinated  pharmacological effect is terminated through hepatic metabolism  Possible Common Mechanism of Action -ability to alter movement of chloride ions across neuronal membranes  Therapeutic Uses Group as a whole has limited therapeutic use.    www.indiandentalacadmey.com
  7. 7.  Doxapram and Nikithamide - used to counteract postanesthetic respiratory depression and for acute hypercapnia in chronic pulmonary disease.  Pentylenetetrazole - used clinically as a tool for screening latent epileptics and experimentally to screen compounds for anti-epileptic activity.  Picrotoxin - used to study CNS mechanisms; it interferes with pathways that are strychnine resistant. www.indiandentalacadmey.com
  8. 8.  Strychnine is a source of accidental poisoning. Also used to study CNS mechanism because of its relatively specific action as a glycine antagonist.  Adverse Reactions: Convulsion is characterized by opisthotonos, i.e., tonic extension of body and all limbs. Back is arched and only the back of the head and the heels are touching the touching the surface. All sensory stimuli produce exaggerated response and slight sensory stimulation may trigger convulsion. www.indiandentalacadmey.com
  9. 9. www.indiandentalacadmey.com
  10. 10. Treatment of Strychnine Poisoning (1) Remove/reduce external sensory stimuli (2) Diazepam or Clonazepam I.V. or nitrous oxide by inhalation to depress CNS and stop convulsions which can be fatal www.indiandentalacadmey.com
  11. 11. PSYCHOMOTOR STIMULANTS  Drugs of Primary Importance Amphetamine - prototype Methamphetamine Methylphenidate www.indiandentalacadmey.com
  12. 12. CHARACTERISTICS  all compounds are absorbed well orally  large portion of untransformed amphetamine is excreted unchanged  in the urine. Consequently, acidifying the urine with ammonium chloride hastens its clearance, and thus reduces its reabsorption in the renal tubules.  Overdose: hyperreflexia, tremors and convulsions  Fatalities: hyperthermia rather than cardiovascular effects www.indiandentalacadmey.com
  13. 13. Pharmacological Actions  The primary effects of an oral dose are wakefulness, alertness, decrease fatigue; mood elevation, increased ability to concentrate; an increase in motor and speech activity. Amphetamines also diminish the awareness of fatigue; person may push exertion to the point of severe damage or even death. www.indiandentalacadmey.com
  14. 14.  Stimulate the respiratory center, especially when respiration is depressed by centrally acting drugs, (barbiturates and alcohol).  Amphetamine can reverse the marked sedation and behavioral retardation resulting from reserpine-like drug.  Depresses appetite by their action on the lateral hypothalamus rather than an effect on metabolic rate. www.indiandentalacadmey.com
  15. 15. Mechanisms of Action  Releases monoamines at synapses in the brain and spinal cord.  Inhibits neuronal uptake of monoamine  Direct agonist of DA and 5-HT receptors  Antagonist at certain adrenreceptors  May inhibit monoamine oxidase. www.indiandentalacadmey.com
  16. 16. Therapeutic Uses  Hyperkinesias - Methylphenidate  Narcolepsy - Amphetamine or methylphenidate  Obesity - Fenfluramine www.indiandentalacadmey.com
  17. 17. Adverse Effects  CNS: Euphoria, dizziness, tremor, irritability, insomnia, Convulsion (at higher doses), hyperthermia and coma  C.V. Cardiac stimulation leads to headache, palpitations, cardiac arrhythmias, anginal pain  Other: Weight loss, Psychotic Reaction which are often misdiagnosed as schizophrenia.  Addiction - including psychic dependence, tolerance and physical dependence. www.indiandentalacadmey.com
  18. 18.  Drug Interactions:    Tricyclic antidepressant Antihypertensive Agents Foods high in tyramine content www.indiandentalacadmey.com
  19. 19. METHYLXANTINES  Caffeine:    Coffee (100-150 mg/cup) Tea (30-40 mg/cups) Cocoa (15-18mg/cup)  Theophylline: Tea and cocoa  Theobromine: Cocoa www.indiandentalacadmey.com
  20. 20. Mechanisms of Action  Increase cyclic nucleotide concentration  Blocks adenosine receptors  Alters intracellular calcium distribution www.indiandentalacadmey.com
  21. 21.  Caffeine, the most widely used drug in the world, is a stimulant. Commonly found in coffee, tea, soft drinks, chocolate and a wide variety of overthe-counter medications, it is legal to buy and easily accessible.  Caffeine is a physically addictive drug www.indiandentalacadmey.com
  22. 22. Pharmacological Activity/ Adverse Effects  Low Doses: 50-250mg/Caffeine (Oral Doses) Increase mental alertness, decrease drowsiness Lessen fatigue  Larger Doses: 250-600mg/Caffeine Irritability, restlessness, tremor, insomnia, headache, palpitations and hyperesthesia GIT upset  Large Doses: > 1000 mg Overt excitement, delirium and clonic seizures www.indiandentalacadmey.com
  23. 23.  Cardiovascular System: Increase rate and force of the heart by directly stimulating myocardium (low doses) Tachycardia and arrhythmias at higher doses. Peripheral vasodilation decease in blood pressure (acute administration) Hypotension and cardiac arrest (rapid i.v. theophyline) www.indiandentalacadmey.com
  24. 24.  Smooth Muscles: Relaxes vascular smooth muscle (Theophylline »Caffeine)  Kidney: All xanthines are capable of producing some degree of diuresis in humans (Theophylline > Caffeine)  Miscellaneous: Xanthines shorten clotting time by increasing tissue prothrombin and factor V. www.indiandentalacadmey.com
  25. 25. Adverse effects  Stimulate gastric secretions in patients with ulcer  Dehydration in children due to vomiting and transient diuretic action (theophyline)  Allergic reaction (aminophylline)  Psychic Dependence (Caffeine) www.indiandentalacadmey.com
  26. 26. Therapeutic Uses  Caffeine + plus ergot alkaloid (Ergotamine): used to treat migraine headaches  OTC preparations: Theophylline: Prophylaxis for chronic asthma Respiratory Stimulant Bronchodilator for relief of asthmatic symptoms www.indiandentalacadmey.com
  27. 27. NICOTINE  CNS Effects:  Powerful CNS stimulant at lower doses; Large doses produce clonic convulsion, then depress CNS, compounding postictal depression  Stimulates respiration  Produces emesis  Tolerance to central actions with chronic use www.indiandentalacadmey.com
  28. 28.  Cardiovascular Effects Tachycardia Increased blood pressure Pupillary constriction Cardiovascular collapse - due to CNS depression  Ganglionic blockade and arrhythmias Fatalities: Due to respiratory failure     www.indiandentalacadmey.com
  29. 29. COCAINE  Psychomotor stimulant  local anesthetic  Chemistry- alkaloid from coca plant alkaloid is highly lipid-soluble hydrochloride salt is water soluble www.indiandentalacadmey.com
  30. 30. Routes of Administration  Chewing: with an-alkaloid material (South America)  Sniffing: hydrochloride salt -absorption: nasal mucous membranes -local vasoconstriction slows absorption and prolongs effect  Oral: large doses are needed for effect rapid onset  Smoking: cocaine is converted to alkaloid (freebase or "crack") which is readily volatilized undegraded at lower temperature. I.V. and smoking: reaches CNS in seconds in high concentration produces more immediate and intense effects www.indiandentalacadmey.com
  31. 31. Pharmacokinetics large vol. of distribution quickly metabolized: half-life 30-90 minutes principal metabolites: a) Ecogonine methylester - inactive b) Benzoylecogonine inactive c) norcocaine - active  half lives of metabolites: 4 to 6 hrs. metabolites: Excreted in urine  Drug Testing: BE - detectable for 1-3 days Cocaine - detectable for a few hours    www.indiandentalacadmey.com
  32. 32. www.indiandentalacadmey.com
  33. 33. www.indiandentalacademy.com Leader in continuing dental education www.indiandentalacadmey.com

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