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PHARMACOLO GY

CNS OVERVIEW
Daripada Abu Hurairah r.a, daripada Nabi SAW bersabda maksudnya: Sesiapa yang melepaskan sesuatu kesusahan seorang mukmin dari kesusahan-kesusahan dunia Allah akan melepaskan darinya satu kesusahan dari kesusahan hari Akhirat dan sesiapa melapangkan seorang yang berada di dalam kesempitan Allah akan melapangkan untuknya di dunia dan di akhirat dan sesiapa yang menutup keburukan saudaranya maka Allah akan menutup keburukannya di dunia dan akhirat dan Allah pasti menolong hamba-Nya selagi mana hambanya menolong saudaranya. Dan sesiapa mengikuti satu jalan untuk mencari ilmu Allah akan memudahkan untuknya jalan ke syurga. Tidak berkumpul satu kaum di dalam rumah dari rumah-rumah Allah dan saling belajar dan mengajar antara satu sama lain melainkan turunlah ketenangan atas mereka, rahmat meliputi mereka, para malaikat mengerumuni mereka dan Allah akan menyebut (nama-nama) mereka di sisi-Nya. Dan sesiapa yang kurang amalannya maka nasab (keturunannya) tidak akan dapat menyempurnakannya. (Muslim) by:

Muhammad Shahir Bin Rahmat

ANXIOLYTIC & SEDATIVE-HYPNOTIC DRUGS


CLASSIFICATION Act on GABA Benzodiazepine Barbiturates Zolpidem Benzodiazepine Sub-Groups Subclass / T Long acting > 24 hrs Intermediate acting = 6-24 hrs Short acting < 6 hrs Drugs Diazepam, clorazepate, chlordiazepoxide & clonazepam all have active metabolite except nitrazepam Lorazepam, temazepam & oxazepam all have no active metabolite except alprazolam Triazolam & midazolam DRUGS

*toxicity of benzodiazepine is treated with Flumazenil Barbiturates Sub-Groups Subclass / T Long acting 10-12 hrs Intermediate active 6-8 hrs Short acting 3-4 hrs Ultrashort acting 15 mins Drugs Phenobarbital & mephobarbital Butabarbital, talbutal, amobarbital Pentobarbital & sarcobarbital Thiopental sodium & methohexital sodium

Other sedative

Buspirone, paraldehyde, chloral hydrate, meprobomate & glutethimide Drugs with other major use but with sedative action : antihistamines -adrenergic blockers (pass BBB) clonidine antidepressants

ANTIEPILEPTIC DRUGS

CLASSIFICATION

DRUGS

Block Na Channels

Potentiate action of GABA Block Ca channels Inhibit glutamate activity

Phenytoin Carbamazepine Oxcarbazepine, lamotrigine & topiramate Valproic acid, benzodiazepine Phenobarbitone & primidone topiramate Ethosuximide, trimethadione Felbamate

ANALGESIC DRUGS
GROUPS Narcotic Analgesic (Opiod) CLASSIFICATIONS 1. Phenanthrene alkaloids opium 2. Semisynthetic morphine derivatives 3. Synthetic morphine substitute 4. Mixed agonist antagonist narcotics analgesic 1. Sialicylic derivatives 2. Aniline derivatives 3. Indole derivatives 4. Phenyl acetic acids 5. Proprionic acids 6. Fenamic acids 7. Oxicams 8. Pyrazolones 9. Others DRUGS Morphine & codeine Diacetyl morphine, dihydromorphine, oxymorphine, oxycodone & dihydrocodeinone Meperidine, fentanyl, methadone & dextropropoxyphene Pentazocine, nalbuphine, buprenorphine & butorphanol Aspirin. sodium salicylate, diflunisal Paracetamol Indomethacin & sulindac Diclofenac, ketorolac & etodolac Ibuprofen, naproxen & ketoprofen Mefenamic acid & flufenamic acid Prioxicam & tenoxicam Phenylbutazone & azapropazone Nabumetone

Non Narcotic Antipyretic Analgesic (Non Steroidal Anti Inflammatory Drugs)

DRUGS OF THERAPIES
DISEASES Rheumatic Fever DRUGS

Salicylate (avoid this drug in rheumatic carditis or cardiac failure) Prenisolone (in rheumatic carditis) Penicilin (Procaine peniciline) Prophylaxis chemoprophylaxis streptococcal infection Penicilin : Benzathine penicilin G or oral penicilin V If sensitive to penicilin : use erythromycin or sulphonamide Acute

Rheumatoid Arthritis

1 Line Drugs nd 2 Line drugs Disease modifying Antirheumatoid Drugs (DMARDs) 3 Line Drugs
rd

st

NSAIDs Methotrexate (chemotherapy) Gold salts (gold Na thiomalate) Penicillamine Hydroxychloroquine Sulphasalazine Immunosuppressive drugs ( Azathioprine & Cyclophosphamide) : indicated in patient with disabling rheumatoid arthritis or systemic manifestation who are refractory to or intolerant to DMARD theraphy Corticosteroids

Gout Prophylaxis Acute Colchicine (Drug of choice) NSAIDs (when colchicine failed) Steroidal anti inflammatory drugs in refractory cases : ACTH, Prednisolone inhibit uric acid synthesis : allopurinol increase UA secretion (uricosuric agents) : Aspirin, Probencid, Sulphinpyrazone & benzbromarone

LESSON ON : PSYCHOTROPIC DRUGS


Selective hypnotic anxiolytic : minor tranquilizer Antipsychotic : neuroleptics, major tranquilizer, antischizophrenic Antidepressant : thymolptics, mood elevating drugs Antimanic : mood stabilizing drugs Psychomotor : psychostimulants Hallucinogenic : psychodysleptic, psychotomimetic drugs Nootropic : drugs enhance mental performances

1.ANTIPSYCHOTIC (ANTISCHIZOPHRENIC) DRUGS

CLASSIFICATION Typical Neuroleptics

DRUGS Phenothiazine aliphatic derivatives : chlorpromazine piperazine derivatives : fluphenazine piperidine derivatives : thioridazine Butyrophenones : haloperidol, droperidol Thioxanthines : flupenthixol, clopenthiol Sulpiride, pimozide, clozapine, risperidone & olanzapine

Atypical Neuroleptics

2.ANTIPARKINSONIAN DRUGS

CLASSIFICATION Anticholinergic Drugs 1. Natural belladona alkaloid 2. Synthetic cholinergic

DRUGS Atropine & hyoscine Trihexyphenidyl (artane) Benztropine (Cogentin) Procyclidine (kemadrin) Biberiden (akineton) Ethopropazine Diphenydramine Orphenadrine (disipal) Levodopa (L-dopa) Amantadine

Drugs That Increase Dopaminergic

3. Phenothiazine with anticholinergic properties 4. Drugs with both anticholinergic & antihistaminic properties 1. Replete neuronal dopamine 2. Increase release dopamine from the stores and inhibit reuptake

Activity

3. Inhibit dopamine metabolism selectively 4. Dopamine agonist

MAOBi : sellegline (deprenyl) COMTi : tolcapone & entacapone Ergot : bromocriptine, perglide & luseride Non ergot : pramipexole & ropinirole

3.ANTIDEPRESSANT DRUGS (THYMOLEPTIC-MOOD ELEVATING DRUGS)


CLASSIFICATION Tricyclic Antidepressant (TCA) MAOI SSRIs Atypical Antidepressants nd (2 Generation Drugs) DRUGS Imipramine, desipramine & amitriptyline Tranylcypromine, phenelzine & isocarboxazide Fluoxetine, fluvoxamine, paroxetine & sertraline Maprotiline

Electroconvulsive theraphy (ECT) is very effective & act more rapid than antidepressants

4.ANTIMANIC (MOOD STABILIZING DRUGS) Lithium Carbonate

LESSON ON : ANESTHETICS
PREANESTHETIC MEDICATION

CLASSIFICATION Sedative hypnotics & Antianxiety Opioid analgesic Anticholinergic Drugs reduce acidity and volume of gastric contents Antiemitics & anthistaminics Anesthetic adjuvants Diazepam

DRUGS

Meperidine Atropine, scopolamine Ranitidine & antacids NM blockers Narcotics

Vasopressor drugs Preanesthetic medication Controlled hypotension : trimetaphan in neuro and plastic surgery Hypothermic : chlorpromazine in cardiosurgery

GENERAL ANESTHETICS

CLASSIFICATION Inhalation

DRUGS Volatile liquids : Halogenated anesthetic : halothane, enflurane, isoflurane, methoxyflurance, desflurance, sevoflurane chloroform & trichloroethylene Ether : diethyl ether & divineyl ether Gases : Nitrous oxide & cyclopropane Ultrashort acting barbiturates : Na thiopentone & methohexitoe Benzodiazepines (diazepam, midazolam) Ketamine (dissociative anesthesia) Etomidate Propofol Opioid analgesic : morphine, fentanyl & fentanyl congeners Neuroleptalanalgesia

Intravenous

Basal anesthesia

Balanced anesthesia

Definition : light anesthesia not deep enough to permit surgical operation not used as sole agents for surgical anesthesia d/t : I. hard to adjust depth & duration of anesthesia II. cant remove excess once they reached the blood III. depend on state of health of metabolizing and excreting organs e.g : diazepam, thiopentone, paraldehyde Definition : combination different drugs to take each drugs beneficial effects while minimizing each agents adverse effects These drugs include : I. pre anesthetic agents II. induction anesthesia : IV --> more rapid induction III. maintenance anesthesia : using inhalation anesthesia IV. NM relaxants : facilitate intubation & relaxation of muscles

LOCAL ANESTHETICS

CLASSIFICATION According to solubility & therapeutic application Soluble LA suitable for injection

DRUGS Procaine, dibucaine, lidocaine & tetracaine all produce surface anesthesia except procaine Particularly on eye

Soluble LA suitable for

topical use Low solubility LA

According to chemical structure

Esters

Amides

Cocaine HCL, phenacaine HCL Benzocaine Use as surface anesthetics as powders & ointments for wound and ulcers Ester of benzoic acid : cocaine Ester of P-aminobenzoic acid : procaine, benzocaine & tetracaine Lidocaine (xylocaine, ligocaine) prilocaine, mepivacaine (carbocaine) & dibucaine

LESSON ON : cns stimulants


CEREBRAL CORTEX STIMULANTS BRAIN STEM STIMULANTS (ANALEPTICS) Xanthines, methylphenidate, cocaine, ephedrine, amphetamine & atropine Direct Megimide Pentylene tetrazole (cardiazole, leptazole) Picrotoxin Lobeline Nikethamide (coramine) Ethamivan (emivan) Amiphenazole (Daptazole) Doxapram (dopram) Carbogen

Indirect Dual

SPINAL CORD STIMULANTS

Strychnine

DRUGS ABUSE

opioids barbiturates & other sedatives hypnotics including alcohol CNS stimulants : caffeine, cocaine & aphetamine hallucinogen : lysergic acid diethylamide (LSD) & phencyclidine (PCP, angle dust) marijuana (cannabis) inhalants : ether, chloroform, industrial solvents like gasoline, pint thinner, glueshoe polish and organics nitrites