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This document provides an overview of neuropharmacology and various central nervous system agents that act on the brain and spinal cord. It discusses the two main branches of neuropharmacology - behavioural and molecular neuropharmacology. It then covers various drug classes that act on the central nervous system including sedatives/hypnotics like benzodiazepines, barbiturates, and cholinergic drugs. Specific drugs are discussed in terms of their mechanisms of action, indications, dosages, and side effects. The document concludes with nursing responsibilities when administering these central nervous system agents.

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Presented By Mr. Pradeepsingh N B Asst.Professor HOD OF Medical –Surgical Nursing
INTRODUCTION  Neuropharmacalogy is the study of how drugs affect cellular function in the body, the nervous system and neural mechanism through which they influence behavior.  Neuropharmacology is a region of science that encompasses many aspects of nervous system from single neuron manipulation to entire areas of brain,spinal cord, and peripheral nerves.  There are two main branches of neuropharmacology: BEHAVIOURAL MOLECULAR
BEHAVIOURAL NEUROPHARMACOLGY  It focuses on the study of how drugs affect human behavior, including the study of how drug dependence and addiction affect the human behavior.
MOLECULAR NEUROPHARMOLOGY It involves the study of neurons and their neurochemical interactions, with the overall goal of developing drugs that have beneficial effects on neurological function.
CENTRAL NERVOUS SYSTEM AGENTS
 Central nervous system agents are medicines that affect the CNS.  The CNS is responsible for processing and controlling most of our bodily functions and consist of nerves in brain & spinal cord.  The drugs that work on CNS include: Analgesics and anti pyretics Anesthetics Hypnotics and sedatives Cholinergic drugs Anticholinergic drugs Muscle relaxants Antipsychotic drugs
Antidepressants Anticonvulsants Adrenergic drugs Mood stabilizing agents Acetylcholine Antiemetics Antiparkinson Central Nervous System stimulants
SEDATIVES AND HYPNOTICS
SEDATIVE S It is a drug that produces calming or quietening effect and reduces excitement, it may induce drowsiness. Drugs that calm the patient and reduce anxiety without inducing normal sleep.
HYPNOTICS It is a drug that induces sleep, resembling natural sleep. Drugs that initiate and maintain normal sleep.
CLASSIFICATION
BENZODIAZEPIN ES
PHARMACOLOGICAL ACTION  Sedation and hypnosis  Reduction in anxiety  Anaesthesia  Muscle relaxation  Anticonvulsion effect  Amnesia  Other actions such as decrease in nocturnal gastric secretion and prevents stress ulcers.
DOSE/ ROUTE/FREQUENCY • 0.25mg – 1mg , TID , oral • Maximum dose – 4mg/day Alprazolam • 5mg – 25mg , TID/QID , oral • Maximum dose – 100mg/day Chlordiazepoxide • 0.5mg – 1mg , TID , oral • Maximum dose – 20mg/day Clonazepam • 5mg – 25mg , TID/QID , oral • Maximum dose – 40mg/day Diazepam • 0.5mg – 1mg , TID/QID , oral. Lorazepam • 10mg – 30mg , TID/QID , oral • Maximum dose – 120mg/day Oxazepam
MECHANISM OF ACTION
PHARMACOKINETICS  Benzodiazepines are completely absorbed on oral administration.  Intramuscular absorption is slow, hence oral route is preferred.  They are extremely bound to plasma protein metabolized in the liver & excreted through kidney.
ADVERSE EFFECTS
CLASSIFICATION BARBITURATES ULTRA SHORT ACTING (< 15-20min) -Theopentone - Melhohexitone SHORT ACTING (< 3hours) -Hexobarbitone - Pentobarbitone - Secobarbitone LONG ACTING (6-12hours) - Mephobarbitone - Phenobarbitone
DOSE / ROUTE / FREQUENCY 1. Mephobarbitol : 32mg – 100mg TID/QID oral 2. Pentobarbitol : For trouble sleeping – 100mg OD (night) oral For sedation before surgery - 100mg before surgery oral 3. Phenobarbitol : Troubled sleeping – 100mg-320mg OD (night) oral Sedation before surgery – 3.5mg/kg body weight 4. Secobarbitol : 200mg-300mg before surgery, oral 100mg for troubled sleep
PHARMACOLOGICAL ACTION 1. CNS: Produce dose dependent effect. - Hypnotics dose shortens the time taken to fall asleep and increases duration. - Sedative dose given at day time can produce drowsiness, reduction in anxiety and excitability. - No analgesic effect but can cause hyperalgesia - Anticonvulsant property.
2. Other systems - Respiratory: Depressed in higher dose. - CVS: Slight decrease in BP and heart rate. - Skeletal muscle: Hypnotic dose has a little effect but anaesthesia dose reduces muscle contraction by action on neuromuscular junction. - Smooth muscle: Tone and motility of bowel is decreased by hypnotic dose. - Kidney: Tend to reduce urine flow.
PHARMACOKINETICS  Barbiturates are well absorbed from the GI tract and widely distributed in the body.  The rate of entry into CNS depends on the lipid solubility.  Redistribution from CNS to skeletal muscle.  Metabolized in the liver by oxidation, dealkylation and conjugation.  Metabolites are excreted in urine.
INDICATIONS  Except for phenobarbitone in epilepsy and thiopentone in anesthesia no other barbiturates are used now.  Used in psychosomatic disorders.  Hypnotics and anxiolytics.
ADVERSE EFFECTS HANGOVER DRUG TOLERANCE HALLUCINATIONS
MISCELLANEOUS 1. PARALDEHYDE - It is a colorless, transparent, pungent, inflammable liquid. - It is an irritant and can dissolve plastic syringe. - It also has anticonvulsant properties.  ROUTE - Rectal - Intra muscular - Oral  USES - As a convulsant in status epilepticus particularly in children - Hypnotic rarely used.
2. MELATONIN - The hormone secreted by the pineal gland is known to regulate sleep. - Melatonin acts on the melatonin receptors. - It doesnot depress the CNS, it improves the quality of sleep and helps in withdrawing benzodiazepines after long term use. 3. RAMELTEON - It is an agonist at the melatonin receptors is a novel hypnotic drug. - It doesnot modify the sleep. - The duration of action is prolonged. - Adverse effects are dizziness and fatigue.
NURSES RESPONSIBILITIES  Nursing considerations for benzodiazepines involve: - Careful monitoring of the patient’s condition - Education of the medication regimen  Benzodiazepines are a schedule IV drug, so the patient should be assessed for drug abuse potential and dependence.  These drugs are a pregnancy risk.  Since benzodiazepines change intraocular pressure, patients with narrow angle glaucoma should not receive these drugs.  Liver and kidney function should also be monitored.  Respiratory depression may result if patient is taking other CNS depressants.
 Common side effects include drowsiness and dizziness.  If a patient receives an overdose of benzodiazepines should be administered to reverse the CNS depression.  All forms of nicotin should be avoided because they decrease the effectiveness of benzodiazepines.  Rebound seizures may develop if the drug is abruptly stopped.  The drug should be taken with food to prevent GI disturbance.  Do not mix these drugs with others because they tend to precipitate and irritate the  Patient teaching should include avoiding alcohol, drugs, herbal medications without prescription.
CHOLINERGIC DRUGS
INTRODUCTION  Cholinergic drugs are drugs that inhibit, enhance or mimic the action of neurotransmitter acetylcholine, the primary transmitter of nerve impulses within the parasympathetic nervous system.  Parasympathetic nervous system is a part of autonomic nervous system that controls smooth muscles, dilates blood vessels, increases bodily secretions and slows the heart rate.
CHOLINERGIC DRUGS DIRECT ACTING - Acetylcholine - Bethanechol - Carbachol - Methacholine - Pilocarpine INDIRECT ACTING REVERSIBLE LIPID SOLUBLE - Physiostigmine - Tacrine - Donepzil - Revastigmine WATER SOLUBLE - Neostigmine - Pyridostigmine - Endophorium IRREVERSIBLE ORGANO-PHOSPHATE - Melathion - Parathion - Chloropyrifos CARBAMATES - Carbaryl - Aldecarb
DIRECT ACTING CHOLINERGICS  These agents mimic the effect of acetylcholine by binding directly to the cholinoreceptors.  They are synthetic esters of choline such as carbachol and bethanechol or naturally occurring alkaloids such as pilocarpine.  All these drugs have longer duration than acetylcholine.
1. ACETYLCHOLINE  It is a neurotransmitter of parasympathetic nervous system and cholinergic nerves. ACTION • Decreases heart rate and cardiac output. • Decreases blood pressure due to vasodilation OTHER ACTIONS - GIT: Increases salivary secretion and increases intestinal motility & secretion. - Respiration: Stimulates bronchiolar secretions. - Genitourinary tract: Increases detrusor muscle tone. - Eye: Miosis (marked constriction of pupil)
Corneal Swelling Bradycardia Hypotension Breathing difficulty Sweating SIDE EFFECTS OF ACETYLCHOLINE
2. BETHANECHOL  Structurally related to ACH, has a strong muscarinic activity.  It directly stimulates muscarinic receptors of GIT causing increase intestinal motility & tone. USES • Bladder stimulation in postpartum & post operative non obstructive urine retention.
Sweating Salivation Hypotension Nausea Diarrhoea Bronchospasm Abdominal pain
3. PILOCARPINE  Mainly used in ophthalmology, it exhibit muscarinic activity, it produces rapid miosis & contraction of the ciliary muscle. USES • It is a drug of choice in the emergency lowering of intra-ocular pressure in case of glaucoma. SIDE EFFECTS - It can enter the brain and cause CNS disturbance. - It stimulates profuse sweating. - Salivation
INDIRECT ACTING CHOLINERGIC DRUGS  These are drugs that exert cholinergic actions by prolonging the life time of acetylcholine via the inhibition of acetyl-cholinesterase enzyme.  This results in accumulation of ACH in synaptic space and provokes response at all cholinoceptors in the body as well as neuromuscular junction and the brain.  These drugs are termed reversible and irreversible.
REVERSIBLE ANTICHOLINERGICS PHYSOSTIGMINE NEOSTIGMINE PYRIDOSTIGMINE
EYE: Glaucoma, accommodative esotropia URINARY TRACT: Neurogenic bladder GASTROINTESTINAL TRACT: Postoperative atony NEUROMUSCULAR JUNCTION: Myasthenia gravis THERAPEUTIC USES OF CHOLINOMIMETICS
 It is reversible inhibitor of acetylcholinesterase and potentiate cholinergic activity throughout body.  It stimulates muscarinic & nicotinic receptors of autonomic nervous system, its duration of action is 2-4 hours, it can enter & stimulate CNS.
Bladder atony Glaucoma Overdose of anticholinergic drugs
BRADYCARDIA CONVULSIONS Skeletal muscle paralysis due to inhibition of ACHesterase at NMJ and ACH accumulation SIDE EFFECTS OF PHYSOSTIGMINE
 Synthetic compound reversibly inhibits acetylcholinesterase, it doesnot enter the CNS.  It has greater effect on skeletal muscle that can increase contractibility then paralysis. USES • Stimulates atonic bladder & intestines • Antidote for neuromuscular blocking agents • Symptomatic treatment in myasthenia gravis
Salivation Hypotension Abdominal pain Diarrhoea Bronchospasm Nausea SIDE EFFECTS OF NEOSTIGMINE
 These are synthetic organophosphorus compounds that bind acetylcholinesterase covalently and inhibit it irreversibly, so there will be increase in ACH at all sites of its release.  These drugs are extremely toxic & used in military as nerve agents.  Some agents like parathion and Malathion are used in insecticides.
 These drug causes permanent inactivation of acetylcholinesterase, the restoration of enzyme activity requires synthesis of new enzymes.  It causes generalized cholinergic stimulation, paralysis of motor function leading to breathing difficulties, convulsions.  The inhibited acetylcholinesterase can be reactivated by pralidoxime which is a synthetic compound that can regenerate new enzyme. CLINICAL USES • Ointment used topically for the treatment of glaucoma, its effect may last for one week after a single administration. • Echothiophate has also the same uses of Isoflurophate.
 Acute intoxication which must be recognized & treated properly.  The dominant initial signs are: - Miosis - Salivation - Sweating - Brochial constriction - Vomiting - Diarrhoea  Cognitive disturbances, convulsions & coma usually follow rapidly.
TREATMENT 1. Maintainance of vital signs, Respiration may be impaired. 2. Atropine parenterally in large doses given as often as required to control signs of muscarinic excess. 3. Therapy often also includes treatment with pralidoxime & administration of benzodiazepines for seizures.
 Administer oral drug on empty stomach to decrease nausea and vomiting  If drug is given intra venously, administer slowly to avoid severe cholinergic effects.  Maintain atropine as standby to use it as an antidote for excessive doses of cholinergic drugs.  Discontinue drud if excessive salivation, diarrhea, emesis or frequent urination becomes a problem to decrease the risk of adverse reactions.  Provide safety precautions of the patients reports poor visual activity in dim light to prevent injury.  Provide comfort measures.  Provide patient education about drug effects and warning signs.
 Anticholinergics are drugs that block the action of acetylcholine. USES Urinary incontinence Overactive bladder Chronic Obstructive Pulmonary Disorder Parkinson’s disease
Anticholinergic drugs Atropine Cyclopentolate Dicyclomine Fesoterodine Hyoxyamine Oxyluitynin Trospium
Myasthenia Gravis Hyperthyroidism Glaucoma Enlarged Prostate Down Syndrome CONTRAINDICATIONS OF ANTICHOLINERGICS
SIDE EFFECTS OF ANTICHOLINERGIC DRUGS
 Assess the consciousness level of the patient before administering the drug.  Monitor for the signs of anticholinergic crisis.  Provide comfort measures for dryness of mucous membranes.  Minimise exposure to heat or cold or strenuous exercise.  Monitor input and output chart.
 Monitor patient for abdominal distension and auscultate for bowel sounds.  Prevent adverse drug reactions.  Provide patient and family education.  Emphasize the importance of adequate fluid and salt intake.
MUSCLE RELAXANTS  These are the drugs that relax muscles.  These are used to reduce discomfort in acute, painful musculoskeletal disorders such as muscle spasms. CLASSIFICATION MUSCLE RELAXANTS Centrally acting muscle relaxants Direct acting muscle relaxants
 These drugs act on central nervous system to interfere with the reflexes that cause muscle spasms.  These drugs include : - Baclofen - Caridoprodol
Indications Trigeminal neuralgia Spasuity Dose 5 mg, TID Contraindications Skeletal muscle spasms due to cerebral palsy Parkinson’s disease Side effects Dizziness Nausea Vomiting Headache Confusion
Indications Relief of discomfort from acute, painful musculoskeletal conditions Dose 350mg, QID Side effects Dizziness Headache Nausea & Vomiting Dyspnea Tachycardia Abdominal cramps
DIRECT ACTING MUSCLE RELAXANTS  These drugs affect peripheral muscle contraction. DANTROBENE Indications Cerebral palsy Multiple sclerosis Muscular dystrophy Polio Tetanus Dose 25 – 100 mg, QID Contraindications Allergy Hepatic disease Side effects Drowsiness Dizziness Diarrhoea Constipation Insomnia Headache
 Monitor patients response to drug.  Provide thorough teaching to the patient about drug, its effects and its side effects.  Explain the patient to avoid alcohol or other depressants while taking medications.  Evaluate the patient for therapeutic response.  Explain the patient that drowsiness usually diminishes with continued therapy.  Instruct the patient to change position slowly which helps to prevent dizziness.  Discontinue the drug if any signs of hypersensitivity are seen.  Screen patient for cardiac depression, pregnancy, lactation or epilepsy.
 Antipsychotic drugs are used to manage psychosis including delusions, paranoia and hallucinations.  They are also known as neuroleptics or major tranquilizers.
• 40 – 800 mg/day Chlorpromazine • 6 – 30 mg/day Thiothixene • 1 – 100 mg/day Haloperidol • 300 – 900 mg/day Clozapine • 20 – 250 mg/day Loxapine • 4 – 8 mg/day Risperidone
MECHANISM OF ACTION
Treatment of acute and chronic psychosis. Selected agents are used as antiemetics. Treatments of hiccoughs. Vocal utterances in Tourette’s disorder.
CONTRAINDICATIONS Hypersensitivity CNS depression Parkinson’s disease Liver, renal and cardiac insufficiency
Dry mouth Constipation Delirium Urinary Retention Orthostatic hypotension
 Risk for other directed violence related to panic anxiety & mistrust of others.  Risk for injury related to medication side effects of sedation, extra pyramidal symptoms, tardive dyskinesia.  Client is instructed not to abruptly stand to prevent fall due to orthostatic hypotension.  Check vitals before and after medication.  Increased intake of fluid& high fibre diet is recommended to avoid dry mouth and constipation.  Educate client to wear full sleeves and eye gears while going out to avoid photosensitivity.
ANTI DEPRESSANTS  Anti depressants are used in the treatment of major depression with psychotic symptoms, alcoholism, schizophrenia or mental retardation.  These drugs elevate mood and alleviate other symptoms associated with moderate to severe depression.
• 50 – 300 mg/day Amitreptyline • 25 – 300 mg/day Doxepin • 200 – 450 mg/day Bupropion • 150 – 500 mg/day Trazodone • 20 – 60 mg/day Citalopram • 20 – 80 mg/day Fluoxetine • 200 – 600 mg/day Nefazodone • 45 – 90 mg/day Phenelzine
INDICATIONS OF ANTIDEPRESSANTS Unipolar or bipolar disorder Generalized anxiety disorder Hypochondriasis Post traumatic stress disorder Bulimia Nervosa
SIDE EFFECTS OF ANTI DEPRESSANTS Sedation Dry mouth Sexual dysfunction Insomnia Weight gain
CONTRAINDICATIONS OF ANTIDEPRESSANTS Hypersensitivity Pheochromocytoma ( tumor on adrenal gland ) Cardiac arrhythmias Hyperthyroidism
NURSE’S RESPONSIBILITIES  Risk for suicide related to depressive mood.  Risk for injury related to side effects of sedation, photosensitivity, arrhythmias, etc.  Socially isolated related to depressive mood.  Constipation related to side effects of the medication.
ANTICONVULSANTS  Treatment of convulsions varies with the type of seizures.  Anticonvulsants inhibit neuromuscular transmission, they may be used for : I. Long term management of chronic epilepsy (recurrent seizures) II. Short term management of acute seizures III. Emergency treatment of status epilepticus (continuous seizures)
Hydantoins Barbiturates Benzodiazepines Succinimides Sulphonamides Classification of anticonvulsants
• 100mg BD Phenytoin • 200 – 400 mg TDS Carbamazepine • 200 mg TDS Sodium valproate • 50 mg/day Lamotrigine • 0.5 – 5 mg/day Clonazepam
MECHANISM OF ACTION  Anticonvulsants suppress the excessive rapid firing of neurons during seizures.  Anticonvulsants also prevent the spread of seizure within the brain.
INDICATIONS OF ANTICONVULSANTS Psychomotor seizures Alcohol withdrawal syndrome Cardiac arrhythmias Status epilepticus seizures during surgery Mixed seizures
CONTRAINDICATIONS OF ANTICONVULSANTS Respiratory obstructions Hematologic disorders Hepatic dysfunctions Complete heart block History of bone marrow suppression
SIDE EFFECTS OF ANTICONVULSANTS Nausea Muscle and joint pain Respiratory depression Megaloblastic anemia Numbness Alopecia
NURSE’S RESPONSIBILITIES  Excessive use of alcohol should be reduced for the efficacy of the drug.  Give oral drugs with meal to minimize gastric irritation.  Prolonged use may led to drug tolerance.  Advice periodic ophthalmologic examinations, because drug can produce ocular damage.  Note that confusion, agitation and behavioral disturbances occurs commonly in elderly people.  Use cautiously in patients having hepatic and cardiac diseases and in elderly and pregnant women.
MOOD STABILIZERS  Mood stabilizers are the drugs used to treat mood disorders, generally characterized by rapid unstable mood shifts alternating between mania & depression.  Mood stabilizers are more effective in mania than the depressive phase of illness.
CLASSIFICATION Lithium • Best known mood stabilizers Anticonvulsants • Carbamazepine • Sodium valproate Antipsychotics • Risperdone • Topiramate
INDICATIONS  Bipolar disorder  Manic depressive psychosis  Recurrent mania  Cyclic depression  Acute hypomania DRUGS INCLUDE : o Lithium carbonate (Li2CO3) o Lithium Chloride (LiCl)
CONTRAINDICATIONS OF MOOD STABILIZERS Pregnancy Cardivascular disorders Kidney disorders Severe dehydration Obesity Diabetes
SIDE EFFECTS OF MOOD STABILIZERS CNS : - Headache - Drowsiness - Slurred speech - Confusion CARDIOVASCULAR : - Hypotension - Arrhythmias GIT : - Dry mouth - Metallic taste - Nausea - Diarrhea
NURSE’S RESPONSIBILITIES  Assess the client’s mood & behavior before & during the course of Lithium therapy & monitor mood change.  Prepare the patient for respected side effects in non-anxious manner.  Monitor serum lithium levels weekly two three times for first 2 months & afterwards once weekly.  Monitor input & output and promote fluid intake of 2-3 L/day to prevent retention.  Assess the weight & check for edema in legs, ankles & wrists, monitor for weight plan.
ANTI EMETIC DRUGS  Antiemetic drugs are medicines that ease nausea & vomiting.  The feeling of nausea results froma complex process in the body and this is why various drugs have been designed to ease nausea in different situations. SOME OF THE ANTI EMETICS ARE : o Sodium citrate o Orthophosphoric acid o Bismuth subsalicylate o Prochlorperazine o Dexamethasone o Ondansetron
INDICATIONS OF ANTI EMETICS Motion sickness Stomach flu Pregnancy Effects of surgery Chemotherapy
Sleepiness Dry mouth Constipation Indigestion Tinnitus SIDE EFFECTS OF ANTI EMETICS
NURSE’S RESPONSIBILITIES  Monitor for dehydration.  Advise patient to have bland foods and avoid spicy foods.  Advise patient to move less and sit upright.  Assess the type of emesis from the patient.  Assess the consciousness level of patient before administering the drug.  Teach patient to change positions slowly.  Assess patients neurological status, level of orientation and reflexes.
ANTIPARKINSONIAM DRUGS INTRODUCTION  Parkinsonism is a chronic, progressive motor disorder characterized by rigidity, tremors, hypokinesis.  If these symptoms worsen, there maybe breathing difficulty and inability to walk.
DRUG DOSE 2 – 3 g/day, BD, Oral. - Symptoms of hypokinesia, rigidity and tremors resolve on administration of Levodopa.
Dizziness Nausea Dark coloured urine Unusual dreams Loss of apetite Abdominal cramps SIDE EFFECTS OF LEVODOPA
DRUG DOSE - 75 – 100 mg, TID, Oral. ACTION - Treat Parkinson’s symptoms such as : • Shakiness • Stiffness • Difficulty in moving
SIDE EFFECTS OF CARBIDOPA Dizziness Loss of apetite Constipation Dry mouth Confusion
NURSE’S RESPONSIBILITIES  Assess for parkinsoniam and extra pyramidal symptoms.  Caution patient to make position change slowly.  Administer drug with low protein foods.  Assess for suicidal tendencies.  Assess for consciousness level of patient before administering drug.  Patient should be taught not to discontinue antiparkinson drugs suddenly.
CNS STIMULANTS INTRODUCTION  CNS stimulants are medicines that stimulate the brain, speeding up both mental and physical processes.  They increase energy , improve attention and alertness and elevate blood pressure, heart rate & respiration rate.
1. AMPHETAMINES  DRUG DOSE - 5 – 10 mg/day, Oral - They promote release of catecholamines from presynaptic nerve terminals & prevent their reuptake into nerve endings.  INDICATIONS - Obesity - Neurolepsy brain dysfunction syndrome in children.
CONTRAINDICATIONS OF AMPHETAMINES Cardiovascular diseases Hypertension Hyperthyroidism Arteriosclerosis Glaucoma
SIDE EFFECTS OF AMPHETAMINES Dizziness Headache Tachycardia Hypertension Diarrhea
NURSE’S RESPONSIBILITIES  Carefully screen potential uses for a history of drug abuse.  Administer last dose atleast 6 hours before bedtime.  Inform diabetic patient that insulin/dietary requirement maybe diluted by amphetamines.  Caution patient that ability to drive or operate heavy machinery maybe impaired by the drug.  Use amphetamines for weight control only after other weight reduction programme have failed.
Conclusion

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neurological drugs.pptx

  • 1.
    Presented By Mr. PradeepsinghN B Asst.Professor HOD OF Medical –Surgical Nursing
  • 2.
    INTRODUCTION  Neuropharmacalogy isthe study of how drugs affect cellular function in the body, the nervous system and neural mechanism through which they influence behavior.  Neuropharmacology is a region of science that encompasses many aspects of nervous system from single neuron manipulation to entire areas of brain,spinal cord, and peripheral nerves.  There are two main branches of neuropharmacology: BEHAVIOURAL MOLECULAR
  • 3.
    BEHAVIOURAL NEUROPHARMACOLGY  It focuseson the study of how drugs affect human behavior, including the study of how drug dependence and addiction affect the human behavior.
  • 4.
    MOLECULAR NEUROPHARMOLOGY It involvesthe study of neurons and their neurochemical interactions, with the overall goal of developing drugs that have beneficial effects on neurological function.
  • 5.
  • 6.
     Central nervoussystem agents are medicines that affect the CNS.  The CNS is responsible for processing and controlling most of our bodily functions and consist of nerves in brain & spinal cord.  The drugs that work on CNS include: Analgesics and anti pyretics Anesthetics Hypnotics and sedatives Cholinergic drugs Anticholinergic drugs Muscle relaxants Antipsychotic drugs
  • 7.
    Antidepressants Anticonvulsants Adrenergic drugs Mood stabilizingagents Acetylcholine Antiemetics Antiparkinson Central Nervous System stimulants
  • 8.
  • 9.
    SEDATIVE S It is adrug that produces calming or quietening effect and reduces excitement, it may induce drowsiness. Drugs that calm the patient and reduce anxiety without inducing normal sleep.
  • 10.
    HYPNOTICS It is adrug that induces sleep, resembling natural sleep. Drugs that initiate and maintain normal sleep.
  • 11.
  • 12.
  • 13.
    PHARMACOLOGICAL ACTION  Sedation andhypnosis  Reduction in anxiety  Anaesthesia  Muscle relaxation  Anticonvulsion effect  Amnesia  Other actions such as decrease in nocturnal gastric secretion and prevents stress ulcers.
  • 14.
    DOSE/ ROUTE/FREQUENCY • 0.25mg– 1mg , TID , oral • Maximum dose – 4mg/day Alprazolam • 5mg – 25mg , TID/QID , oral • Maximum dose – 100mg/day Chlordiazepoxide • 0.5mg – 1mg , TID , oral • Maximum dose – 20mg/day Clonazepam • 5mg – 25mg , TID/QID , oral • Maximum dose – 40mg/day Diazepam • 0.5mg – 1mg , TID/QID , oral. Lorazepam • 10mg – 30mg , TID/QID , oral • Maximum dose – 120mg/day Oxazepam
  • 15.
  • 16.
    PHARMACOKINETICS  Benzodiazepines arecompletely absorbed on oral administration.  Intramuscular absorption is slow, hence oral route is preferred.  They are extremely bound to plasma protein metabolized in the liver & excreted through kidney.
  • 17.
  • 18.
    CLASSIFICATION BARBITURATES ULTRA SHORT ACTING (<15-20min) -Theopentone - Melhohexitone SHORT ACTING (< 3hours) -Hexobarbitone - Pentobarbitone - Secobarbitone LONG ACTING (6-12hours) - Mephobarbitone - Phenobarbitone
  • 19.
    DOSE / ROUTE/ FREQUENCY 1. Mephobarbitol : 32mg – 100mg TID/QID oral 2. Pentobarbitol : For trouble sleeping – 100mg OD (night) oral For sedation before surgery - 100mg before surgery oral 3. Phenobarbitol : Troubled sleeping – 100mg-320mg OD (night) oral Sedation before surgery – 3.5mg/kg body weight 4. Secobarbitol : 200mg-300mg before surgery, oral 100mg for troubled sleep
  • 20.
    PHARMACOLOGICAL ACTION 1. CNS:Produce dose dependent effect. - Hypnotics dose shortens the time taken to fall asleep and increases duration. - Sedative dose given at day time can produce drowsiness, reduction in anxiety and excitability. - No analgesic effect but can cause hyperalgesia - Anticonvulsant property.
  • 21.
    2. Other systems -Respiratory: Depressed in higher dose. - CVS: Slight decrease in BP and heart rate. - Skeletal muscle: Hypnotic dose has a little effect but anaesthesia dose reduces muscle contraction by action on neuromuscular junction. - Smooth muscle: Tone and motility of bowel is decreased by hypnotic dose. - Kidney: Tend to reduce urine flow.
  • 22.
    PHARMACOKINETICS  Barbiturates arewell absorbed from the GI tract and widely distributed in the body.  The rate of entry into CNS depends on the lipid solubility.  Redistribution from CNS to skeletal muscle.  Metabolized in the liver by oxidation, dealkylation and conjugation.  Metabolites are excreted in urine.
  • 23.
    INDICATIONS  Except forphenobarbitone in epilepsy and thiopentone in anesthesia no other barbiturates are used now.  Used in psychosomatic disorders.  Hypnotics and anxiolytics.
  • 24.
  • 25.
    MISCELLANEOUS 1. PARALDEHYDE - Itis a colorless, transparent, pungent, inflammable liquid. - It is an irritant and can dissolve plastic syringe. - It also has anticonvulsant properties.  ROUTE - Rectal - Intra muscular - Oral  USES - As a convulsant in status epilepticus particularly in children - Hypnotic rarely used.
  • 26.
    2. MELATONIN - Thehormone secreted by the pineal gland is known to regulate sleep. - Melatonin acts on the melatonin receptors. - It doesnot depress the CNS, it improves the quality of sleep and helps in withdrawing benzodiazepines after long term use. 3. RAMELTEON - It is an agonist at the melatonin receptors is a novel hypnotic drug. - It doesnot modify the sleep. - The duration of action is prolonged. - Adverse effects are dizziness and fatigue.
  • 27.
    NURSES RESPONSIBILITIES  Nursing considerationsfor benzodiazepines involve: - Careful monitoring of the patient’s condition - Education of the medication regimen  Benzodiazepines are a schedule IV drug, so the patient should be assessed for drug abuse potential and dependence.  These drugs are a pregnancy risk.  Since benzodiazepines change intraocular pressure, patients with narrow angle glaucoma should not receive these drugs.  Liver and kidney function should also be monitored.  Respiratory depression may result if patient is taking other CNS depressants.
  • 28.
     Common sideeffects include drowsiness and dizziness.  If a patient receives an overdose of benzodiazepines should be administered to reverse the CNS depression.  All forms of nicotin should be avoided because they decrease the effectiveness of benzodiazepines.  Rebound seizures may develop if the drug is abruptly stopped.  The drug should be taken with food to prevent GI disturbance.  Do not mix these drugs with others because they tend to precipitate and irritate the  Patient teaching should include avoiding alcohol, drugs, herbal medications without prescription.
  • 29.
  • 30.
    INTRODUCTION  Cholinergic drugsare drugs that inhibit, enhance or mimic the action of neurotransmitter acetylcholine, the primary transmitter of nerve impulses within the parasympathetic nervous system.  Parasympathetic nervous system is a part of autonomic nervous system that controls smooth muscles, dilates blood vessels, increases bodily secretions and slows the heart rate.
  • 31.
    CHOLINERGIC DRUGS DIRECT ACTING -Acetylcholine - Bethanechol - Carbachol - Methacholine - Pilocarpine INDIRECT ACTING REVERSIBLE LIPID SOLUBLE - Physiostigmine - Tacrine - Donepzil - Revastigmine WATER SOLUBLE - Neostigmine - Pyridostigmine - Endophorium IRREVERSIBLE ORGANO-PHOSPHATE - Melathion - Parathion - Chloropyrifos CARBAMATES - Carbaryl - Aldecarb
  • 32.
    DIRECT ACTING CHOLINERGICS  Theseagents mimic the effect of acetylcholine by binding directly to the cholinoreceptors.  They are synthetic esters of choline such as carbachol and bethanechol or naturally occurring alkaloids such as pilocarpine.  All these drugs have longer duration than acetylcholine.
  • 33.
    1. ACETYLCHOLINE  Itis a neurotransmitter of parasympathetic nervous system and cholinergic nerves. ACTION • Decreases heart rate and cardiac output. • Decreases blood pressure due to vasodilation OTHER ACTIONS - GIT: Increases salivary secretion and increases intestinal motility & secretion. - Respiration: Stimulates bronchiolar secretions. - Genitourinary tract: Increases detrusor muscle tone. - Eye: Miosis (marked constriction of pupil)
  • 34.
    Corneal Swelling Bradycardia Hypotension Breathingdifficulty Sweating SIDE EFFECTS OF ACETYLCHOLINE
  • 35.
    2. BETHANECHOL  Structurallyrelated to ACH, has a strong muscarinic activity.  It directly stimulates muscarinic receptors of GIT causing increase intestinal motility & tone. USES • Bladder stimulation in postpartum & post operative non obstructive urine retention.
  • 36.
  • 37.
    3. PILOCARPINE  Mainlyused in ophthalmology, it exhibit muscarinic activity, it produces rapid miosis & contraction of the ciliary muscle. USES • It is a drug of choice in the emergency lowering of intra-ocular pressure in case of glaucoma. SIDE EFFECTS - It can enter the brain and cause CNS disturbance. - It stimulates profuse sweating. - Salivation
  • 38.
    INDIRECT ACTING CHOLINERGIC DRUGS These are drugs that exert cholinergic actions by prolonging the life time of acetylcholine via the inhibition of acetyl-cholinesterase enzyme.  This results in accumulation of ACH in synaptic space and provokes response at all cholinoceptors in the body as well as neuromuscular junction and the brain.  These drugs are termed reversible and irreversible.
  • 39.
  • 40.
    EYE: Glaucoma, accommodative esotropia URINARY TRACT: Neurogenicbladder GASTROINTESTINAL TRACT: Postoperative atony NEUROMUSCULAR JUNCTION: Myasthenia gravis THERAPEUTIC USES OF CHOLINOMIMETICS
  • 41.
     It isreversible inhibitor of acetylcholinesterase and potentiate cholinergic activity throughout body.  It stimulates muscarinic & nicotinic receptors of autonomic nervous system, its duration of action is 2-4 hours, it can enter & stimulate CNS.
  • 42.
    Bladder atony GlaucomaOverdose of anticholinergic drugs
  • 43.
    BRADYCARDIA CONVULSIONS Skeletal muscle paralysis dueto inhibition of ACHesterase at NMJ and ACH accumulation SIDE EFFECTS OF PHYSOSTIGMINE
  • 44.
     Synthetic compoundreversibly inhibits acetylcholinesterase, it doesnot enter the CNS.  It has greater effect on skeletal muscle that can increase contractibility then paralysis. USES • Stimulates atonic bladder & intestines • Antidote for neuromuscular blocking agents • Symptomatic treatment in myasthenia gravis
  • 45.
    Salivation Hypotension Abdominalpain Diarrhoea Bronchospasm Nausea SIDE EFFECTS OF NEOSTIGMINE
  • 46.
     These aresynthetic organophosphorus compounds that bind acetylcholinesterase covalently and inhibit it irreversibly, so there will be increase in ACH at all sites of its release.  These drugs are extremely toxic & used in military as nerve agents.  Some agents like parathion and Malathion are used in insecticides.
  • 47.
     These drugcauses permanent inactivation of acetylcholinesterase, the restoration of enzyme activity requires synthesis of new enzymes.  It causes generalized cholinergic stimulation, paralysis of motor function leading to breathing difficulties, convulsions.  The inhibited acetylcholinesterase can be reactivated by pralidoxime which is a synthetic compound that can regenerate new enzyme. CLINICAL USES • Ointment used topically for the treatment of glaucoma, its effect may last for one week after a single administration. • Echothiophate has also the same uses of Isoflurophate.
  • 48.
     Acute intoxicationwhich must be recognized & treated properly.  The dominant initial signs are: - Miosis - Salivation - Sweating - Brochial constriction - Vomiting - Diarrhoea  Cognitive disturbances, convulsions & coma usually follow rapidly.
  • 49.
    TREATMENT 1. Maintainance ofvital signs, Respiration may be impaired. 2. Atropine parenterally in large doses given as often as required to control signs of muscarinic excess. 3. Therapy often also includes treatment with pralidoxime & administration of benzodiazepines for seizures.
  • 50.
     Administer oraldrug on empty stomach to decrease nausea and vomiting  If drug is given intra venously, administer slowly to avoid severe cholinergic effects.  Maintain atropine as standby to use it as an antidote for excessive doses of cholinergic drugs.  Discontinue drud if excessive salivation, diarrhea, emesis or frequent urination becomes a problem to decrease the risk of adverse reactions.  Provide safety precautions of the patients reports poor visual activity in dim light to prevent injury.  Provide comfort measures.  Provide patient education about drug effects and warning signs.
  • 52.
     Anticholinergics aredrugs that block the action of acetylcholine. USES Urinary incontinence Overactive bladder Chronic Obstructive Pulmonary Disorder Parkinson’s disease
  • 53.
  • 54.
  • 55.
    SIDE EFFECTS OFANTICHOLINERGIC DRUGS
  • 56.
     Assess theconsciousness level of the patient before administering the drug.  Monitor for the signs of anticholinergic crisis.  Provide comfort measures for dryness of mucous membranes.  Minimise exposure to heat or cold or strenuous exercise.  Monitor input and output chart.
  • 57.
     Monitor patientfor abdominal distension and auscultate for bowel sounds.  Prevent adverse drug reactions.  Provide patient and family education.  Emphasize the importance of adequate fluid and salt intake.
  • 58.
    MUSCLE RELAXANTS  Theseare the drugs that relax muscles.  These are used to reduce discomfort in acute, painful musculoskeletal disorders such as muscle spasms. CLASSIFICATION MUSCLE RELAXANTS Centrally acting muscle relaxants Direct acting muscle relaxants
  • 59.
     These drugsact on central nervous system to interfere with the reflexes that cause muscle spasms.  These drugs include : - Baclofen - Caridoprodol
  • 60.
    Indications Trigeminal neuralgia Spasuity Dose 5 mg, TID Contraindications Skeletalmuscle spasms due to cerebral palsy Parkinson’s disease Side effects Dizziness Nausea Vomiting Headache Confusion
  • 61.
    Indications Relief of discomfort fromacute, painful musculoskeletal conditions Dose 350mg, QID Side effects Dizziness Headache Nausea & Vomiting Dyspnea Tachycardia Abdominal cramps
  • 62.
    DIRECT ACTING MUSCLERELAXANTS  These drugs affect peripheral muscle contraction. DANTROBENE Indications Cerebral palsy Multiple sclerosis Muscular dystrophy Polio Tetanus Dose 25 – 100 mg, QID Contraindications Allergy Hepatic disease Side effects Drowsiness Dizziness Diarrhoea Constipation Insomnia Headache
  • 63.
     Monitor patientsresponse to drug.  Provide thorough teaching to the patient about drug, its effects and its side effects.  Explain the patient to avoid alcohol or other depressants while taking medications.  Evaluate the patient for therapeutic response.  Explain the patient that drowsiness usually diminishes with continued therapy.  Instruct the patient to change position slowly which helps to prevent dizziness.  Discontinue the drug if any signs of hypersensitivity are seen.  Screen patient for cardiac depression, pregnancy, lactation or epilepsy.
  • 64.
     Antipsychotic drugsare used to manage psychosis including delusions, paranoia and hallucinations.  They are also known as neuroleptics or major tranquilizers.
  • 65.
    • 40 –800 mg/day Chlorpromazine • 6 – 30 mg/day Thiothixene • 1 – 100 mg/day Haloperidol • 300 – 900 mg/day Clozapine • 20 – 250 mg/day Loxapine • 4 – 8 mg/day Risperidone
  • 67.
  • 68.
    Treatment of acuteand chronic psychosis. Selected agents are used as antiemetics. Treatments of hiccoughs. Vocal utterances in Tourette’s disorder.
  • 69.
    CONTRAINDICATIONS Hypersensitivity CNS depressionParkinson’s disease Liver, renal and cardiac insufficiency
  • 70.
    Dry mouth ConstipationDelirium Urinary Retention Orthostatic hypotension
  • 71.
     Risk forother directed violence related to panic anxiety & mistrust of others.  Risk for injury related to medication side effects of sedation, extra pyramidal symptoms, tardive dyskinesia.  Client is instructed not to abruptly stand to prevent fall due to orthostatic hypotension.  Check vitals before and after medication.  Increased intake of fluid& high fibre diet is recommended to avoid dry mouth and constipation.  Educate client to wear full sleeves and eye gears while going out to avoid photosensitivity.
  • 72.
    ANTI DEPRESSANTS  Antidepressants are used in the treatment of major depression with psychotic symptoms, alcoholism, schizophrenia or mental retardation.  These drugs elevate mood and alleviate other symptoms associated with moderate to severe depression.
  • 73.
    • 50 –300 mg/day Amitreptyline • 25 – 300 mg/day Doxepin • 200 – 450 mg/day Bupropion • 150 – 500 mg/day Trazodone • 20 – 60 mg/day Citalopram • 20 – 80 mg/day Fluoxetine • 200 – 600 mg/day Nefazodone • 45 – 90 mg/day Phenelzine
  • 74.
    INDICATIONS OF ANTIDEPRESSANTS Unipolaror bipolar disorder Generalized anxiety disorder Hypochondriasis Post traumatic stress disorder Bulimia Nervosa
  • 75.
    SIDE EFFECTS OFANTI DEPRESSANTS Sedation Dry mouth Sexual dysfunction Insomnia Weight gain
  • 76.
    CONTRAINDICATIONS OF ANTIDEPRESSANTS Hypersensitivity Pheochromocytoma (tumor on adrenal gland ) Cardiac arrhythmias Hyperthyroidism
  • 77.
    NURSE’S RESPONSIBILITIES  Riskfor suicide related to depressive mood.  Risk for injury related to side effects of sedation, photosensitivity, arrhythmias, etc.  Socially isolated related to depressive mood.  Constipation related to side effects of the medication.
  • 78.
    ANTICONVULSANTS  Treatment ofconvulsions varies with the type of seizures.  Anticonvulsants inhibit neuromuscular transmission, they may be used for : I. Long term management of chronic epilepsy (recurrent seizures) II. Short term management of acute seizures III. Emergency treatment of status epilepticus (continuous seizures)
  • 79.
  • 80.
    • 100mg BD Phenytoin •200 – 400 mg TDS Carbamazepine • 200 mg TDS Sodium valproate • 50 mg/day Lamotrigine • 0.5 – 5 mg/day Clonazepam
  • 81.
    MECHANISM OF ACTION Anticonvulsants suppress the excessive rapid firing of neurons during seizures.  Anticonvulsants also prevent the spread of seizure within the brain.
  • 82.
  • 83.
  • 84.
    SIDE EFFECTS OFANTICONVULSANTS Nausea Muscle and joint pain Respiratory depression Megaloblastic anemia Numbness Alopecia
  • 85.
    NURSE’S RESPONSIBILITIES  Excessiveuse of alcohol should be reduced for the efficacy of the drug.  Give oral drugs with meal to minimize gastric irritation.  Prolonged use may led to drug tolerance.  Advice periodic ophthalmologic examinations, because drug can produce ocular damage.  Note that confusion, agitation and behavioral disturbances occurs commonly in elderly people.  Use cautiously in patients having hepatic and cardiac diseases and in elderly and pregnant women.
  • 86.
    MOOD STABILIZERS  Moodstabilizers are the drugs used to treat mood disorders, generally characterized by rapid unstable mood shifts alternating between mania & depression.  Mood stabilizers are more effective in mania than the depressive phase of illness.
  • 87.
    CLASSIFICATION Lithium • Best knownmood stabilizers Anticonvulsants • Carbamazepine • Sodium valproate Antipsychotics • Risperdone • Topiramate
  • 89.
    INDICATIONS  Bipolar disorder Manic depressive psychosis  Recurrent mania  Cyclic depression  Acute hypomania DRUGS INCLUDE : o Lithium carbonate (Li2CO3) o Lithium Chloride (LiCl)
  • 90.
    CONTRAINDICATIONS OF MOODSTABILIZERS Pregnancy Cardivascular disorders Kidney disorders Severe dehydration Obesity Diabetes
  • 91.
    SIDE EFFECTS OFMOOD STABILIZERS CNS : - Headache - Drowsiness - Slurred speech - Confusion CARDIOVASCULAR : - Hypotension - Arrhythmias GIT : - Dry mouth - Metallic taste - Nausea - Diarrhea
  • 92.
    NURSE’S RESPONSIBILITIES  Assessthe client’s mood & behavior before & during the course of Lithium therapy & monitor mood change.  Prepare the patient for respected side effects in non-anxious manner.  Monitor serum lithium levels weekly two three times for first 2 months & afterwards once weekly.  Monitor input & output and promote fluid intake of 2-3 L/day to prevent retention.  Assess the weight & check for edema in legs, ankles & wrists, monitor for weight plan.
  • 93.
    ANTI EMETIC DRUGS Antiemetic drugs are medicines that ease nausea & vomiting.  The feeling of nausea results froma complex process in the body and this is why various drugs have been designed to ease nausea in different situations. SOME OF THE ANTI EMETICS ARE : o Sodium citrate o Orthophosphoric acid o Bismuth subsalicylate o Prochlorperazine o Dexamethasone o Ondansetron
  • 95.
    INDICATIONS OF ANTIEMETICS Motion sickness Stomach flu Pregnancy Effects of surgery Chemotherapy
  • 96.
    Sleepiness Dry mouthConstipation Indigestion Tinnitus SIDE EFFECTS OF ANTI EMETICS
  • 97.
    NURSE’S RESPONSIBILITIES  Monitorfor dehydration.  Advise patient to have bland foods and avoid spicy foods.  Advise patient to move less and sit upright.  Assess the type of emesis from the patient.  Assess the consciousness level of patient before administering the drug.  Teach patient to change positions slowly.  Assess patients neurological status, level of orientation and reflexes.
  • 98.
    ANTIPARKINSONIAM DRUGS INTRODUCTION  Parkinsonismis a chronic, progressive motor disorder characterized by rigidity, tremors, hypokinesis.  If these symptoms worsen, there maybe breathing difficulty and inability to walk.
  • 99.
    DRUG DOSE 2 –3 g/day, BD, Oral. - Symptoms of hypokinesia, rigidity and tremors resolve on administration of Levodopa.
  • 100.
    Dizziness Nausea Darkcoloured urine Unusual dreams Loss of apetite Abdominal cramps SIDE EFFECTS OF LEVODOPA
  • 101.
    DRUG DOSE - 75– 100 mg, TID, Oral. ACTION - Treat Parkinson’s symptoms such as : • Shakiness • Stiffness • Difficulty in moving
  • 102.
    SIDE EFFECTS OFCARBIDOPA Dizziness Loss of apetite Constipation Dry mouth Confusion
  • 103.
    NURSE’S RESPONSIBILITIES  Assessfor parkinsoniam and extra pyramidal symptoms.  Caution patient to make position change slowly.  Administer drug with low protein foods.  Assess for suicidal tendencies.  Assess for consciousness level of patient before administering drug.  Patient should be taught not to discontinue antiparkinson drugs suddenly.
  • 104.
    CNS STIMULANTS INTRODUCTION  CNSstimulants are medicines that stimulate the brain, speeding up both mental and physical processes.  They increase energy , improve attention and alertness and elevate blood pressure, heart rate & respiration rate.
  • 105.
    1. AMPHETAMINES  DRUGDOSE - 5 – 10 mg/day, Oral - They promote release of catecholamines from presynaptic nerve terminals & prevent their reuptake into nerve endings.  INDICATIONS - Obesity - Neurolepsy brain dysfunction syndrome in children.
  • 106.
  • 107.
    SIDE EFFECTS OFAMPHETAMINES Dizziness Headache Tachycardia Hypertension Diarrhea
  • 108.
    NURSE’S RESPONSIBILITIES  Carefullyscreen potential uses for a history of drug abuse.  Administer last dose atleast 6 hours before bedtime.  Inform diabetic patient that insulin/dietary requirement maybe diluted by amphetamines.  Caution patient that ability to drive or operate heavy machinery maybe impaired by the drug.  Use amphetamines for weight control only after other weight reduction programme have failed.
  • 109.