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Cology Project

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    decrease rate of

    absorption

    Peak Plasma Time:

    1.5-2 hr

    Elimination

    Half-Life: ~5 hr

    acetylcholine), exhibits

    high binding affinity for

    muscarinic M3

    receptors on lacrimal &

    salivary gland

    epithelium: incr

    salivation

    Nicotine - Oral gum, patch for

    smoking

    Agonist at both NN

    and NM receptors

    cessation

    Medical use for

    smoking cessation

    nonmedical use in

    smoking and in

    insecticides

    Activates autonomic

    postganglionic neurons

    (bothsympathetic and

    parasympathetic and

    skeletal

    muscleneuromuscular

    end plates enters CNSand activates NN

    receptor

    Pilocarpine Isopto Carpine Oral lozenge and

    topical

    Like bethanechol,

    partial agonist

    Glau coma; Sjgrens

    syndrome

    Activates M1 through

    M3

    receptors in all

    peripheral

    tissues causes

    increased

    secretion, smooth

    muscle

    contraction (except

    vascular

    smooth muscle

    relaxes), and

    changes in heart rate

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    Varenicline Chantix Absorption

    Completely absorbed

    Bioavailability: High

    Peak plasma time: 3-4

    hr

    Elimination

    Excretion: Urine (92%)

    Half-life: 24 hr

    Excretion: Urine (92%)

    Agonist at nicotinic

    receptors; acts on

    mesolimbic dopamine

    system associated with

    nicotine addiction,

    Smoking Cessation Appetite changes

    Chest pain

    Constipation

    Dry mouth Dyspepsia

    Dyspnea

    Ambenonium Mytelase Poor oral absorption

    Onset: 20-30 min

    Duration: 4-8 hr

    Acetylcholinesterase

    inhibitor;

    Myasthenia Gravis Urinary urgency

    Salivation Vomiting

    Nausea Diarrhea

    Lacrimation, miosis

    Donepezil Aricept AbsorptionBioavailability: 100%

    Peak plasma time: 3-4

    hr

    Elimination

    Half-life: 70 hr

    Acetylcholinesteraseinhibitor

    Alzheimer's Disease Nausea DiarrheaInsomnia Headache

    Vomiting Cramping

    Fatigue

    Edrophonium Tensilon Onset: IV: 30-60 sec;

    IM: 2-10 min

    Duration: IV: 5-10 min;

    IM: 5-45 min

    Inhibits destruction of

    acetylcholine by

    cholinesterase

    Myasthenia Gravis Urinary frequencyWeakness Hypotension

    Arrhythmia BradycardiaLaryngospasm

    Galantamine Reminyl, Razadyne Half-Life: 7 hr

    Peak Plasma Time: 1

    hr

    Increases acetylcholine

    from surviving

    presynaptic nerve

    terminals by modulating

    Alzheimer Disease

    Hepatic Impairment

    Abdominal pain

    Anorexia

    Muscle cramp

    Fatigue Dizziness

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    CHAPTER :8

    TOPIC : Cholinoceptor-Blocking Drugs

    NAME OF THE DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    THERAPEUTIC

    INDICATION

    ADVERSE EFFECT

    Atropine Atreza Metabolism: Liver Half-

    Life: 2.5 hr Absorption:

    90% Onset:

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    Peak plasma time: 7 hr

    Metabolism Liver, by

    CYP3A4 and CYP2D6

    Elimination Half-Life: 13-

    19 hr Excretion: 60%

    urine; 40% feces

    the M3 muscarinic

    receptor; receptor

    blocking limits bladder

    contractions, and

    reduce symptoms of

    bladder

    irritability/overactivity

    Dizziness Dry eyes

    Dyspepsia Nausea

    UTI

    Dicyclomine Bentyl Available in oral and

    parenteral forms short t

    but action lasts up to 6

    hours

    Competitive

    antagonism

    at M3 receptors

    Irritable bowel

    syndrome,

    minor diarrhea

    Reduces smooth

    muscle and secretory

    activity of gut

    Fesoterodine Toviaz Absorption

    Bioavailability: 52%

    Protein Bound: 50% Vd:

    169 L (5-HMT active

    metabolite) Elimination

    Half-Life: 7 hr Excretion:

    Urine (70%); feces (7%)

    Competitive muscarinic

    receptor antagonist;

    inhibition of receptors

    in the bladder prevent

    symptoms of urgency

    and frequency

    Abdominal pain

    Constipation Dyspepsia

    Insomnia Nausea

    Urinary retention ,UTI

    Overactive Bladder

    Flavoxate Urispas Onset: 55 min

    Peak Effect: 112 min

    Excretion: Urine (10-30%)

    Anticholinergic smooth

    muscle relaxant that

    inhibits

    phosphodiesterase and

    counteracts muscle

    spasm in urinary tract;

    nocturia, suprapubic

    pain, urinary

    incontinence, urinary

    tract irritation,

    Abdominal pain Blurred

    vision Confusion

    Constipation

    Disturbance in ocular

    accommodation

    Drowsiness Dry

    Glycopyrrolate Robinul Onset: 1 min (IV); 15-30

    min (IM, SC) Duration: 2-

    3 hr (parenteral, vagal

    Competitively inhibits

    action of ACh on

    autonomic effectors

    Peptic Ulcer Disease Dry mouth Dry skin

    Anhidrosis Flushing

    Blurred vision

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    block); 7 hr (parenteral,

    inhibition of salivation);

    8-12 hr (PO;

    anticholinergic effects)

    innervated by

    postganglionic nerves

    Inhibits salivation,

    tracheobronchial

    secretions,

    bradycardia, and

    hypotension

    Cycloplegia

    Photophobia

    Palpitation

    Xerophthalmia

    Constipation

    Homatropine , Isopto Homatropine N/A Blocks the responses

    of the sphincter muscle

    of iris & ciliary muscle

    of the lens to

    cholinergic stimulation,

    thereby producingmydriasis and

    cycloplegia

    Cycloplegia/Mydriasis

    for Refraction

    Increased IOP

    Follicular conjunctivitis

    Vascular congestion

    Edema Xerostomia

    Burning Irritation

    Stinging Blurred vision

    Thirst

    l-Hyoscyamine Anaspaz, Cystospaz-

    M, Levsin,

    Bioavailability: Tab

    (100%), SR (81%)

    Onset: IV/IM/SC (2-3

    min), SL (5-20 min),

    tab/SR (20-30 min)Duration:IV/IM/SC/tab/SL

    (up to 4 hr), SR (12 hr)

    Peak plasma time:

    Tab/SR (2.5 hr)

    Parasympatholytic,

    atropine-like effects,

    especially peripherally;

    blocks the action of

    acetylcholine atparasympathetic sites

    in smooth muscle,

    secretory glands, and

    CNS

    Gastrointestinal

    Disorders

    Hypermotility of Lower

    Urinary Tract

    Blurred vision

    Constipation

    Dysphagia

    Photosensitivity

    Ipratropium Atrovent Minimal systemic

    absorption

    Anticholinergic

    (parasympatholytic)

    agent; inhibits vagally

    Maintenance treatment

    of bronchospasm,

    including chronic

    Bronchitis (10-23%)

    Chronic obstructive

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    Onset: 15 min

    Duration: 3-4 hr

    Peak plasma time: 1-3 hr

    mediated reflexes by

    antagonizing

    acetylcholine action;

    bronchitis and

    emphysema

    pulmonary disease

    (COPD) exacerbation

    Sinusitis

    Mepenzolate Cantil Absorption: Limited

    Excretion: Urine (3-33%)& feces

    Postganglionic

    parasympathetic

    inhibitor. Inhibits gastric

    acid and pepsin

    secretion and inhibits

    spontaneous

    contractions of the

    colon

    Peptic Ulcer Dizziness Confusion

    Headache Insomnia

    Nervousness

    Weakness Drowsiness

    Tachycardia

    Methscopolamine Pamine Absorption: Incomplete

    Onset of action: 1 hr

    Duration: 4-6hr

    Excretion: Urine,

    unabsorbed drug in

    feces

    Reduces the volume of

    the total acid content of

    gastric secretion,

    reduces gastric

    secretion, and inhibits

    salivation. Peripherally

    blocks muscarinic

    receptors

    Peptic Ulcer Disease Blurred vision

    Cycloplegia Mydriasis

    Headache Dizziness

    Drowsiness Palpitation

    Oxybutynin Ditropan Bioavailability: 6% (~1.5-

    2 times higher for

    extended-release)

    Onset: 30-60

    Exerts antispasmodic

    and antimuscarinic

    effects on smooth

    muscle

    Overactive Bladder Asthenia Dizziness

    Headache Blurred

    vision Dry eyes

    Diarrhea Nausea Pain

    Propantheline Pro-Banthine Bioavailability: PO

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    Onset: 30-45 min (PO)

    Duration: Upt to 6 hr

    (PO)

    parasympathetic

    muscarinic receptor

    sites

    Decreased sweating

    Scopolamine - Transdermal patch for

    mation sickness

    Unknown mechanism

    in CNS

    Prevention of motion

    sickness andpostoperative and

    nausea and vomiting

    Reduces vertigo,

    Postoperative nausea

    Solifenacin Vesicare Bioavailability: 90%

    Peak plasma time: 3-8 hr

    Competitive

    muscarinic-receptor

    antagonist

    Overactive Bladder,

    Urge Incontinence

    Blurred vision

    Tiotropium Spiriva Onset: 30 min Duration:

    >24 hr

    Long-acting

    antimuscarinic agent,often referred to asanticholinergic

    Inhibits M3-receptors atsmooth muscle,leading tobronchodilation

    Chronic Obstructive

    Pulmonary Disease

    Abdominal pain

    Allergic reaction

    Tolterodine Detrol Onset: Overactivebladder, 1 wk; urge

    incontinence, 1 hr

    Competitive muscarinicreceptor antagonist;

    Overactive Bladder,Urge Incontinence

    Blurred visionConstipation Dizziness

    Drowsiness

    Tropicamide Mydriacyl Onset: 15 min

    Maximum effect: 60 min

    Duration: 3 hr

    Blocks acetylcholine

    resulting in relaxation

    of cholinergically

    innervated iris

    Mydriasis Dry mouth

    Nausea

    Vomiting

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    sphincter muscle

    Trospium (Spasmex, Sanctura) Half-life: 20 hr

    (immediate release)

    Peak plasma time: 5-6 hr

    Reduces the smooth

    muscle tone of the

    bladder by

    antagonizing the

    effects of acetyl choline

    on muscarinic

    receptors.

    Overactive Bladder Constipation

    Tachycardia

    Mecamylamine (Inversine Half-Life: 24 hr Onset:

    0.5-2 hr Duration: 6-12 hr

    Excretion: urine 100%

    Ganglionic blocker,

    inhibits acetylcholine at

    autonomic ganglia

    Hypertession Fatigue Sedation

    Constipation

    Pralidoxime Protopam Onset: 5-15 min Binds to

    organophosphates and

    breaks alkyl

    phosphate-

    cholinesterase bond to

    restore activity of

    acetylcholinesterase

    Organophosphate

    Poisoning

    Blurred vision Double

    vision Hypertension

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    CHAPTER :9

    TOPIC :Adrenoreceptor Agonist

    NAME OF THE DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    THERAPEUTIC

    INDICATION

    ADVERSE EFFECTS

    Amphetamine Adderall Well absorbed

    Onset of action: 30-60min

    Duration: 4-6 h

    Sympathomimetic

    amine that promotes

    release of dopamine

    and norepinephrine

    from their storage sites

    in the presynaptic

    nerve terminals

    ADHD Abdominal painHeadache InsomniaLoss of appetite

    Apraclonidine Iopidine Peak Plasma Time: 3-5hr (reduction inintraocular pressure)

    Peak PlasmaConcentration (0.5%admin): 0.9 ng/mL

    Alpha-1 & alpha-2

    adrenergic receptor

    agonist; may reduce

    acqueous humor

    formation

    Glaucoma Discomfort HyperemiaPruritus BlanchingBlurred visionConjunctivitis

    Armodafinil Nuvigil Peak plasma time: 2 hr Unknown; not

    sympathomimetic (R-

    enantiomer of

    modafinil)

    Narcolepsy Nausea

    Dry mouth

    Dizziness Anxiety

    Diarrhea

    Brimonidine Alphagan Metabolized by liver Alpha2 adrenergic Elevated IOP in

    Patients with

    Allergic conjunctivitis

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    Peak plasma time: 1-4

    hr (brimonidine)

    receptor agonist; Glaucoma or Ocular

    Hypertension

    Conjunctival folliculosis

    Conjunctival hyperemia

    Eye pruritus

    Dexmedetomidine Precedex Half-life, elimination: 6min; 2 hr (terminal)

    Peak plasma: 0.3-1.5ng/mL

    Centrally acting alpha2-

    adrenoceptor agonist

    that has sedative and

    anesthetic properties

    possibly by activating

    G-proteins in the

    brainstem

    ICU Sedation Anemia Bradycardia

    Fever Pleural effusion

    Leukocytosis

    Dexmethylphenidate Focalin Bioavailability: 22-25%

    Onset of action: 12hr(extended release)

    The more

    pharmacologically

    active CNS stimulant of

    the d-threo-

    enantiomers; blocks

    reuptake of

    norepinephrine and

    dopamine

    Attention Deficit

    Hyperactivity Disorder

    Abdominal pain

    Headache Insomnia

    Restlessness

    Dextroamphetamine Dexedrine Peak plasma time: ~3hr (immediate release);~8 hr (sustainedrelease)

    Onset of action: 1-1.5hr

    Sympathomimetic

    amine that promotes

    release of dopamine

    and norepinephrine

    from their storage sites

    in the presynaptic

    nerve terminals

    Narcolepsy Vomiting

    Emotional lability

    Nervousness

    Fatigue Fever

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    Dobutamine Dobutrex Intravenous, required

    dose titration to desired

    effect

    Activated adenylyl

    cyclase, increasing

    myocardial contractility

    Cardiogenic shocks

    acute heart failure

    Positive inotropic effect

    Dopamine Intropin Onset: 5 min (adults)

    Duration:

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    to desired effect cyclase relaxation

    Hydroxyamphetamine Paremyd Onset: 15 min

    Maximum effect: 60

    min

    Duration: 3 hr

    Blocks acetylcholine

    resulting in relaxation

    of cholinergicallyinnervated iris

    sphincter muscle

    Mydriasis Tachycardia PallorHeadacheParasympathetic

    stimulation Transientstinging Dry mouth

    Isoproterenol Isuprel Half-Life: 3-7 hr

    Duration: cardiac arrest(IV): 8-50 min

    Strong beta-1 & beta-2

    effects resulting in incr

    CO, decr PVR, &

    variable BP & renal

    perfusion changes

    Adams-Stokes Attacks,

    Cardiac Arrest, or

    Heart Block

    Tachycardia

    Hypertension

    Dysrhythmias

    Angina

    Metaraminol Aramine) Bioavailability: PO,96%

    Duration: Short-acting

    Glucocorticoid; elicits

    mild mineralocorticoid

    activity and moderate

    anti-inflammatory

    effects; controls orprevents inflammation

    by controlling rate of

    protein synthesis,

    Acute Adrenal

    Insufficiency

    Adrenal suppression

    Arthralgia

    Bladder dysfunction

    Cardiomegaly

    Methamphetamine Desoxyn Half-Life: 4-5 hr

    Absorption: Rapid

    Metabolism: Liver

    Amphetamine

    anorexigenic agent;

    sympathomimetic

    amine related to

    Attention Deficit

    Hyperactivity Disorder

    Dizziness, drugtolerance, dysphoricmood, euphoria,headache, insomnia,restlessness, tremor

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    ephedrine and

    amphetamine with CNS

    stimulant activity

    Methylphenidate Ritalin Bioavailability: ~30%;large individualdifferences (11-52%)

    Duration: 3-6 hr (IR); 3-8 hr (ER, SR); 8-12 hr(CD, LA, Concerta)

    Peak plasma time: 6-8hr (PO); 7.5-10.5 hr;(patch)

    Unknown; may block

    reuptake of

    norepinephrine and

    dopamine into

    presynaptic neurons;

    Attention Deficit

    Hyperactivity Disorder

    Headache

    Hypertension

    Nausea

    Nervousness

    Toxic psychosis

    Seizures

    Midodrine ProAmatidine Oral prodrug converted

    to active drug with 1h

    peak effect

    Activated

    phospholipase C.

    resulting in increase

    intracellular calcium

    and vasoconstriction

    Orthostatic

    hypotension

    Vascular Smooth

    muscle contraction

    increasing blood

    pressure

    Modafinil Provigil Peak plasma time: 2-4

    hr

    Unknown; not

    sympathomimetic

    Obstructive Sleep

    Apnea/Hypopnea

    Syndrome (OSAHS)

    Hypotension

    Hypertension

    T-wave changes

    Amnesia

    Anxiety

    Naphazoline Privine Absorption: minimalsystemic

    Alpha 1 adrenergic

    agonist; stimulates

    Nasal Decongestant Burning StingingSneezing Dryness Local

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    Tetrahydrozoline Visine Duration: 2-3hr

    (vasoconstriction)

    May stimulate alpha-

    adrenergic receptors in

    the arterioles of the

    conjunctiva; produces

    vasoconstriction

    Conjunctival

    Congestion

    Irritation/burning

    Blurred vision

    Headache

    Tremor

    Tizanidine Zanaflex Bioavailability: 40%

    Peak serum time: 1-4hr

    Alpha-2 adrenergic

    receptor agonist

    structurally related to

    clonidine; increases

    presynaptic inhibition of

    motor neurons

    Muscle Spasticity Dry mouth

    Somnolence

    Dizziness Asthenia

    Xylometazoline Otrivin Onset: 5-10 min

    Duration: 5-6 hr

    Metabolism: unknown

    Alpha adrenergic

    agonist

    Nasal Congestion Anxiety

    Dizzy

    Tremor

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    CHAPTER :10

    TOPIC :Adrenoreceptor Antagonist

    NAME OF THE DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECT

    Alfuzosin (Uroxatral) Bioavailability: 49%

    Peak Plasma Time: 8

    hr Peak Plasma

    Concentration: 13.6

    ng/mL AUC: 194

    ng.hr/mL

    Selective antagonist of

    postsynaptic alpha-1-

    adrenoceptors;

    Benign Prostatic

    Hyperplasia (BPH)

    Back pain Brochitis

    Constipation Dizziness

    Doxazosin Cardura Bioavailability:

    Immediate release,65%; extended release,

    54-59%

    Blocks alpha1

    receptors in prostaticstromal and bladder

    tissues;

    Benign Prostatic

    Hyperplasia

    Dizziness Fatigue

    Headache

    Phenoxybenzamine Dibenzyline Half-Life: 24 hr Onset:

    several hours

    Alpha blocker,

    noncompetitive alpha-

    adrenergic blockade of

    post ganglionic

    synapses in smoothmuscle, exocrine

    glands

    Hypertension

    Pheochromocytoma

    Tachycardia Dizziness

    Drowsiness Fatigue

    Phentolamine Regitine Half-Life:19 min (IV)

    Duration: 30-45 min

    (IM); 15-30 min (IV)

    Blocks alph-adrenergic

    receptors to briefly

    antagonize circulating

    epinephrine and

    Pheochromocytoma Nasal congestion Post-

    treatment pain Injection

    site pain Diarrhea

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    norepinephrine

    Silodosin Rapaflow Bioavailability: 32%

    Half-Life: 13 +/- 8 hr

    Selective antagonist of

    postsynaptic alpha-1-

    adrenoceptors

    Benign Prostatic

    Hyperplasia

    Diarrhea HeadacheInsomnia Dizziness

    Tamsulosin Flomax Bioavailability: Fasting,30%

    Onset: 4-8 hr

    Tamsulosin is slightly

    selective for 1A

    Benign prostatic

    hyperplasia

    1A

    Blockade may relax

    prostatic smooth

    muscles more

    than vascular smooth

    muscle

    Terazosin Hytrin Bioavailability: 90%

    Onset (hypertension): 3hr

    Blocks postsynapticalpha-1 receptor; alphablockade causesarterial and venousdilation

    Benign Prostate

    Hyperplasia

    HypotensionRhinitis/nasalcongestionLightheadednessSomnolence

    Tolazoline (Priscoline) Bioavailability: ~100%Onset: 30 min

    Duration: 4-6 hr

    Inhibits synthesis ofprostaglandins in body

    tissues by inhibiting at

    least 2 cyclo-

    oxygenase (COX)

    isoenzymes, COX-1

    and COX-2

    Pain Dizziness DyspepsiaEpigastric pain

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    Acebutolol Sectral Oral 12 , with intrinsic

    sympathomimetic

    (partial agonist) effect

    Hypertension

    arrhythmias migraine

    may avoid worsening

    of bradycardia

    Lowers BP modestly

    lower HR

    Atenolol Tenormin Bioavailability: 46-60%Onset:

    Antihypertensiveresponse, 3 hr

    Duration: 12-24 hr(normal renal function)

    Block 1> 2 Angina pectoris

    hypertension

    arrhythmias

    Lower HR and BP

    reduce renin may be

    safer in

    asthma

    Betaxolol Betoptic Onset: Within 30 minDuration: 12 hr

    Block 1> 2 Angina pectoris hypertension

    arrhythmias

    Lower HR and BP reduce renin may be

    safer in asthma

    Bisoprolol Zebeta Half-Life: 9-12 hr

    (normal renal function);

    27-36hr (

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    of bradycardia

    Carvedilol Coreg Bioavailability: 25-35%(immediate release)

    Onset(antihypertensive):Initial response, 1 hr;peak response, 1-2 hr

    Nonselective beta-

    adrenergic and alpha1-

    adrenergic blocking

    agent with no intrinsic

    activity for use in

    congestive heart failure

    and hypertension

    Congestive heart failure Dizziness FatigueHypotension

    Weight gainHyperglycemia

    Esmolol (Brevibloc) Pa renteral only half -

    life ~ 10 min

    1> 2 Rapid control of BP and

    arrhythmias,

    thyrotoxicosis and

    myocardial ischemia

    intraoperatively

    Very brief cardiac

    blockade

    Labetalol Normodyne, Trandate Bioavailability: 25%(PO)

    Onset: PO, 20-120 min;

    IV, 2.5 min

    Nonselective beta

    blocker with intrinsic

    sympathomimetic

    activity; also alphablocker

    Hypertension DizzinessLightheadednessNausea

    Levobunolol (Betagan Liquifilm Peak Plasma Time: 30min

    Onset of action: 1hr

    Peak effect: 2-6hr

    Nonselective beta-

    adrenergic receptor

    blocker; reduces IOP

    by reducing production

    of aqueous humor

    Open-angle Glaucoma Ataxia BurningLethargy DiscomfortBand keratopathy

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    Metipranolol Optipranolol Onset: 30 min Duration:24 hr Maximum effect:2 hr

    Nonselective beta-

    blocker

    Open-Angle Glaucoma Burning sensation ineye , BlepharitisBlurred visionLight intolerance

    Metoprolol Lopressor, Toprol Bioavailability:

    Immediate release, 40-

    50%; extended release,

    65-77% relative to

    immediate release

    Blocks response to

    beta-adrenergic

    stimulation;

    cardioselective for

    beta1 receptors at low

    doses, with little or no

    effect on beta2

    receptors

    Acute Myocardial

    Infarction

    Dizziness Headache

    Tiredness Depression

    Diarrhea

    Nadolol Corgard Oral, parenteral Block 1and 2 Hypertension angina

    pectoris arrhythmias

    migraine

    hyperthyroidism

    Lower HR and BP

    reduce

    renin

    Nebivolol Bystolic Block 1> 2 Angina pectoris

    hypertension

    arrhythmias

    Lower HR and BP

    reduce renin may be

    safer in

    asthma

    Penbutolol Levatol Half-Life: 5 hr Beta adrenergic Arterial Hypertension Aggravate CHF

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    hyperthyroidism

    Metyrosine Demser Half-Life: 3-4 hr

    Bioavailability: Wellabsorbed

    Metabolism: liver

    Inhibits synthesis of

    endogenous

    catecholamines thru

    inhibition of tyrosine

    hydroxylase

    Chronic

    Pheochromocytoma

    DiarrheaExrapyramidalSymptoms

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    CHAPTER 16

    TOPIC :Histamine , Serotonin and Ergot Alkaloids

    NAME OF THE DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECT

    Azelastine Astelin Nasal Onset: 1-3 hr

    Duration: 12 hr

    H1-receptor antagonist;

    inhibits release of

    histamine and other

    mediators involved in

    allergic response

    Seasonal Allergic

    Rhinitis

    Bitter taste

    Headache

    Somnolence

    Cold symptoms/rhinitis

    Cough

    Brompheniramine Brovex Half-Life: 11.8-34.7 hr

    Onset: 30 min

    Histamine H1-receptor

    antagonist

    Perennial & seasonal

    allergic & vasomotor

    rhinitis, relief of

    symptoms from colds,

    urticaria, angioedema,

    anaphylactic reactions,

    pruritus, allergic

    conjunctivitis

    Restlessness,

    insomnia, tremors,

    euphoria, nervousness,

    delirium, palpitation,

    seizures is less

    common

    Buclizine Bucladin-S Softabs

    Carbinoxamine Histex Half-Life: 10-20 hr

    Metabolism: Hepatic

    Excretion: Urine

    Histamine H1-receptor Allergies Dizziness Lassitude

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    Cetirizine Zyrtec Oral duration 12 24 h Competitive

    antagonism/inverse

    agonism at

    H1receptors

    IgE immediate

    allergies, especially hay

    fever, urticaria

    Reduces or prevents

    histamine effects on

    smooth muscle,

    immune cells

    Chlorpheniramine Chlor-Trimeton N/A Chlorpheniramine

    blocks muscle

    responses in histamine

    and acts as an

    antagonism of the

    constrictor effects of

    histamine on

    respiratory smoothmuscle.

    Relief of Cold & Flu

    Symptoms

    Hypotension

    Palpitations

    Tachycardia

    Confusion

    Convulsion

    Clemastine Tavist Onset: 5-7 hr Duration:

    8-12 hr

    Histamine H1-receptor

    antagonist in blood

    vessels, respiratory

    tract, and

    gastrointestinal tract

    Allergic Rhinitis Dizziness Lassitude

    Disturbed coordination

    Muscular weakness

    Diphenhydramine Benadryl Oral and parenteral

    duration 4 6 h

    Competitive

    antagonism/inverse

    agonism at H1

    receptors

    IgE immediate

    allergies, especially hay

    fever, urticaria often

    used as a sedative,

    antiemetic, and anti-

    motion sickness drug

    Reduces or prevents

    histamine effects on

    smooth muscle,

    immune cells also

    blocks muscarinic and

    adrenoceptors

    highly sedative

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    Sumatriptan Imitrex Oral, nasal, parenteral

    duration 2 h

    Partial agonist at

    5-HT1B/1D receptors

    Migraine and cluster

    headache

    Effects not fully

    understood may

    reduce release of

    calcitonin gene-related

    peptide andperivascular edema in

    cerebral circulation

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    CHAPTER :17

    TOPIC : Vasoactive Peptide

    NAME OF THE DRUG BRAND NAME PHARMACOKINETIC MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECT

    Valsartan Diovan Bioavailability: 25%Onset: 2 hr

    Selective competitiveantagonist of

    angiotensin AT1

    receptors

    Hypertension Arteriolar dilation.Decrease aldosterone

    secretion. Increase

    sodium and water

    excretion

    Enalapril Lexxel enalapril: initial 1-4 hr,

    peak 8-18 hr

    Inhibits conversion of

    angiotensin I to

    angiotensin II

    Hypertension heart

    failure

    Arteriolar dilation

    decreased aldosterone

    secretion increased

    sodium and water

    excretion

    Aliskiren Valturna Onset: (valsartan) 2 hr Inhibits catalytic activity

    of renin

    Hypertension Arteriolar dilation

    decreased aldosterone

    secretion increased

    sodium and water

    excretion

    Icatibant Firazyr Bioavailability: 97%

    Peak Plasma Time: 45

    minutes

    Selective antagonist of

    kinin B2

    receptors

    Hereditary angioedema Blocks effects of kinins

    on pain, hyperalgesia,

    and inflammation

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    PO: 60-65% vomiting

    Meclinertant N/A N/A Antagonist of central

    and peripheral

    neurotensin receptors

    None identified Blocks some central

    and peripheral

    (vasodilator) actions of

    neurotensin

    Telcagepant N/A N/A Antagonists of the

    calcitonin gene-related

    peptide (CGRP)

    recepto

    Migraine

    1

    Blocks some central

    and peripheral

    (vasodilator) actions of

    CGRP

    Palosuran N/A N/A Antagonist of urotensin

    receptors

    Diabetic renal failure

    1

    Blocks vasoconstrictor

    action of urotensin

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    CHAPTER :18

    TOPIC : The Eicosanoid , Prostaglandin , thromboxane, Leukotriene , Related compound

    NAME OF THE DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECTS

    Alprostadil Half-Life: 5-10 min Relaxes arterial smoothmuscle, producing

    vasodilation

    Inhibits platelet

    aggregation

    (prostaglandin E1)

    Erectile Dysfunction BradycardiaHypotension Seizures

    Tachycardia

    Bimatoprost Lumigan Absorption: no

    significant systemic

    accumulation

    Half Life: 45 min

    Prostaglandin analog;

    outflow of aqueous

    humor

    Elevated Intraocular

    Pressure

    Ocular dryness (3-10%)

    Visual disturbance

    Carboprost

    tromethamine

    Hemabate Peak plasma time: 20-

    30 min Concentration:

    1-1.6 ng/mL Half-life: 3

    hr

    Inhibits or stimulates

    smooth muscle

    contraction

    Refractory Postpartum

    Uterine Bleeding

    Nervousness Epistaxis

    Sleep disorder

    Dinoprostone Prepidil, Cervidil Onset: In most first and

    second trimester

    pregnancies, slight

    uterine contractions

    begin within 10 min

    Relaxes cervical

    smooth muscle;

    Cervical Ripening Fever/temperature

    elevations (1%)

    GI upset

    Epoprostenol Flolan Half-life: 3-6 min Potent peripheral Pulmonary Jaw pain Headache

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    Metabolism: rapidly

    hydrolyzed in blood to

    metabolites

    vasodilator of all

    vascular beds; also

    prevents platelet

    aggregation

    Hypertension Myalgia

    Iloprost Ventavis) Vd: 0.7-0.8 L/kg Protein

    Bound: 60% Duration:30-60 min

    Synthetic analog of

    prostagladin PGI2

    Pulmonary Arterial

    Hypertension

    Flushing Cough

    Hypotension NauseaHeadache

    Latanoprost Xalatan Absorption: ocular and

    systemic Half-Life: 17

    min

    Prostaglandin F2-alpha

    analog;

    Elevated Intraocular

    Pressure

    Blurred vision Burning

    and stinging Foreign

    body sensation

    Misoprostol Cytotec Onset: 2-3 hr (initial

    response for acid

    secretion) Duration: 3

    hr (inhibition of acid

    secretion)

    Synthetic prostaglandin

    E analogue

    NSAID-Induced Ulcer Anaphylaxis Anemia

    Cardiac dysrhythmia

    Chest pain

    Montelukast Singulair Peak plasma time:

    Tablet, 3-4 hr;

    chewable tablet, 2-2.5

    hr; granules, 1-3 hr

    Blocks binding of

    leukotriene D4 to its

    receptor;

    Asthma Abdominal painEczema InfluenzaLaryngitis Pharyngitis

    Travoprost Travatan Absorption: through thecornea

    Peak Plasma Time:within 30 min

    Prostaglandin F2-alpha

    analog

    Open-Angle Glaucoma Decreased visual acuity(

    Ocular discomfort

    Foreign body sensation

    Pain Pruritus

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    Treprostinil Remodulin Bioavailability: ~100%

    (SC); 64-72%

    (inhalation) Peak

    plasma time: 10 hr

    Peripheral prostacyclin

    vasodilator of both

    pulmonary and

    systemic arterial

    vascular bed

    Pulmonary Arterial

    Hypertension

    Nausea DiarrheaVasodilation

    Jaw pain Rash

    Zafirlukast Accolate Half-Life: 8-16 hrOnset: 3-14 days

    Inhibitsbronchoconstriction as

    competitive receptor

    antagonist of

    leukotrienes D4 & E4

    Asthma Abdominal painInfection Nausea

    Diarrhea Generalized

    pain

    Zileuton Zyflo Half-Life: 2.5 hr Onset:

    2-5 hr

    Inhibitor of 5-

    lipoxygenase, which

    inhibits formation ofLTB4, LTC4, LTD4, &

    LTE4

    Asthma Abdominal pain ALTelevation AstheniaDyspepsia Diarrhea

    Generalized pain

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    CHAPTER :20

    TOPIC : Drug in Asthma

    NAME OF DRUGS BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECTS

    Albuterol Proventil, Ventolin Aerosol inhalation duration several hours

    also available for

    nebulizer and

    parenteral use

    Selective 2agonist Asthma, chronicobstructive pulmonary

    disease (COPD) drug

    of choice in acute

    asthmatic

    bronchospasm

    Asthma prophylaxis

    Prompt, efficaciousbronchodilation

    Albuterol/Ipratropium Combivent Peak plasma time:

    Albuterol, 3 hr (from

    portion swallowed)

    Peak plasma

    concentration:

    Albuterol, 419-802

    pg/mL (from portion

    swallowed)

    Albuterol: Beta2-

    adrenergic

    bronchodilator

    Ipratropium:

    Anticholinergic

    (parasympatholytic)

    agent

    COPD Lung disease

    Headache Dyspnea

    Montelukast Singulair Oral duration hours Block leukotriene D4

    receptors

    Prophylaxis of asthma,

    especially in children

    and in aspirin-induced

    asthma

    Block airway response

    to exercise and antigen

    challenge

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    Zafirlukast Accolate Oral duration hours Block leukotriene D4

    receptors

    Prophylaxis of asthma,

    especially in children

    and in aspirin-induced

    asthma

    Block airway response

    to exercise and antigen

    challenge

    Omalizumab Xolair Parenteral duration 2

    4 d

    Humanized IgE

    antibody reduces

    circulating IgE

    Severe asthma

    inadequately

    controlled by above

    agents

    Reduces frequency of

    asthma exacerbations

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    CHAPTER 23

    TOPIC : The Alcohol

    NAME OF DRUG BRAND NAME PHARMACOKINETIC MECHANISM OF ACTION

    THERAPEUTICINDICATION

    ADVERSE EFFECT

    Chlordiazepoxide HCI Librium

    Diazepam Valium AbsorptionBioavailability: 90%(PR)Duration: Variable,dependent on dose andfrequency (PO[hypnotic action]); 15-60 min (IV [sedativeaction])

    DistributionProtein bound: 98%EliminationHalf-life: 20-70 hr(active metabolite)

    Modulates postsynapticeffects of GABA-Atransmission, resultingin an increase inpresynaptic inhibition.

    Appears to act on partof the limbic system, aswell as on the thalamusand hypothalamus, to

    induce a calming effect

    Alcohol WithdrawalEndoscopyMuscle SpasmSeizure DisorderStatus Epilepticus

    NeutropeniaJaundice MuscleweaknessRespiratory depressionUrinary retentionDepressionIncontinenceBlurred visionDysarthria HeadacheSkin rash

    Lorazepam Ativan Bioavailability: 90%

    Onset: 1-3 min (IV insedation); 15-30 min(IM in hypnosis)Duration: Up to 8 hrPeak plasma time: 2 hr(PO);

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    MetabolismMetabolites: InactiveUndergoes glucuronicacid conjugationEliminationHalf-life: 18 hr (children2-12 years); 42 hr

    (neonates); 28 hr(adolescents); 18 hr(end stage renaldisease); 14 hr (adults)

    and reticular formation Chronic Insomnia

    Oxazepam Serax Half-life elimination:2.8-5.7 hrPeak plasma time: 3 hrPeak plasma

    concentration: 450ng/mLMetabolism: Glucuronicacid conjugationProtein binding: 86-99% Excretion: Urine

    Binds receptors atseveral sites within theCNS, including thelimbic system andreticular formation.Effects may bemediated throughGABA receptor system.Increase in neuronalmembrane permeabilityto chloride ionsenhances the inhibitoryeffects of GABA; theshift in chloride ionscauseshyperpolarization (lessexcitability) andstabilization of thenuronal membrane

    Anxiety Alcohol Withdrawal

    Sedation AtaxiaConfusionMemory impairmentDizziness Drowsiness

    Muscle weaknessSyncope edemaLeukopenia, blooddyscrasias

    Thiamine HCI - Distribution: Distributesmainly to heart, brain,kidney, and liverExcretion: Urine

    Absorption: Adequate

    (PO); rapid and

    Forms thiaminepyrophosphate bycombining withadenosinetriphosphate; essential

    coenzyme in

    WernickeEncephalopathyBeriberiRDA

    Warmth AnaphylaxisCyanosis DiaphoresisRestlessness

    Angioneurotic edemaPruritus Urticaria

    Pulmonary edema

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    complete (IM) carbohydratemetabolism

    WeaknessTightness of the throatNausea

    Acamprosate Campral Protein Bound:NegligibleVd: 1 L/kgPeak PlasmaTime: 3-8hrConcentration: 350ng/mL for a dose of 666mg TIDBioavailability: 11%,decreased by foodMetabolism: NoneExcretion: UrineHalf-life: 20-33 hr

    Not fully understood;may act by interactingwith glutamate & GABAneurotransmitter

    systems

    AlcholismRenal Impairment

    Accidental injury Anorexia Anxiety Asthenia DepressionDizziness Dry mouthFlatulence InsomniaNausea Pain

    Disulfiram Antabuse AbsorptionPeak plasma time: 4 hrPeak plasmaconcentration: 2.4mcg/mLDuration: up to 2 wkOnset: 2-12 hrMetabolismHepatic 80-90%

    Metabolites:DiethyldithiocarbamateEnzymes inhibited:hepatic CYP2C9,CYP2E1EliminationExcretion: Feces andexhaled gases

    Produces sensitivity toEtOH via blocking itsoxidation atacetaldehyde stage,resulting in unpleasantreactions includingpalpitations,hypotension, chestpain, nausea, vertigo,thirst, flushing, and

    nausea

    Alcoholism Fatigue HeadacheImpotenceMetallic aftertaste

    Acneiform eruptionsPolyneuritis RashHepatitisPeripheral neuropathyOptic neuritisPsychotic disorder

    Naltrexone HCI ReVia 96% absorbed fromgastrointestinal tract,but because of first-

    Opioid competitivereceptor antagonist;shows highest affinity

    Opioid Dependence Alcohol Dependence

    Nausea HeadacheDecreased appetite

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    pass metabolism, only5-40% reachessystemic circulation

    for mu receptors;congener ofoxymorphone

    Insomnia VomitingDiarrhea Dizziness

    Ethanol - Metabolism: LiverHalf-life elimination: 15-20 mg/dL/hrExcretion: Urine; lungs

    Vd: 0.6-0.7 L/kg

    Competes withmethanol & ethyleneglycol for alcoholdehydrogenase to

    inhibit production oftoxic metabolites

    Methanol Toxicity,Ethylene GlycolPoisoningTreatment of congenital

    venous and lymphaticmalformations

    IntoxicationFlushing hypotension

    Agitation HypoglycemiaN/V PolyuriaIntoxication

    Fomepizole Antizol Onset of action: 1.5-2hr Vd: 0.6-1.02 L/kgExcretion: Urine

    Inhibits alcoholdehydrogenase, whichcatalyzes themetabolism of ethanol,methanol and ethyleneglycol; has no effectupon CNS or need formonitoring levels (likeEtOH currently)

    Methanol & EthyleneGlycol PoisoningRenal Impairment

    Bad/metallic tasteDizzinessDrowsiness BackacheNystagmus Fever

    Abdominal pain

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    CHAPTER 25

    TOPIC : General Anesthetic

    NAME OF DRUG BRAND NAME PHARMACOKINETIC MECHANISM OF ACTION

    THERAPEUTICINDICATION

    ADVERSE EFFECT

    Desflurane Suprane Onset: 1-2 min Absorption:

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    Droperidol Inapsine Half-Life elimination: 2 hr(parent drug), 8-12 hr(metabolites)Onset: 3-10 min

    Duration: 2-4 hr, maypersist up to12 hr

    dopamine receptorblockade in brain,predominantlydopamine-2 receptor &

    when reuptake isprevented, a strongantidopaminergic,antiserotonic responseoccurs

    Antiemetic , Delirium ,Hepatic and RenalImpairment

    Restlessness AnxietyExtrapyramidalSymptomsDystonic reactionsPseudoparkinsoniansigns and symptomsTardive dyskinesiaSeizure

    Enflurane Ethrane Onset of action: 7-10minutesPeak PlasmaConcentration:

    biotransformation resultsin low serum fluoridelevels (average 15micromol/L); can exceed50 micromol/L ifanesthesia >2 MAC h

    Inhalation anesthetic Anesthesia , Analgesia HypotensionRespiratory depressionHypoxia

    ArrhythmiasShiveringNauseaVomiting

    Etomidate Amidate Onset: Within 60 secDuration: 3-5 min due toredistribution from CNS

    Nonbarbituratehypnotic used for theinduction ofanesthesia; lacksanalgesic activity; hasminimal cardiovasculareffects

    General AnesthesiaInduction

    ArrhythmiasHyperventilationHTNHypotensionHypoventilationLaryngospasmNausea/vomiting

    Fospropofol Lusedra Peak Plasma Time: 2-4min to propofol; 8-12 minof propofol fromfospropofol:Protein Bound: 98%Onset: ~8 min

    Sedative-hypnotic,prodrug of propofol;interacts with GABA Areceptor

    HeadacheHypotensionNausea/vomiting

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    Half-life: 0.8-0.96 hrDuration: ~5 min (time tofully alert)

    Halothane Fluothane 1.08 in neonates to 0.64in the elderly, Addition ofN20 in adults reducesMAC to 0.29%.

    inhalation anestheticHalothane anesthesiaalso causes dilation ofthe vessels of the skin

    and skeletal muscles. Itdoes not cause therelease ofcatecholamines fromadrenergic stores.

    inhalational generalanesthetic,

    Liver damage, heartarrest and abnormalincrease in bodytemperature.

    Isoflurane Forane Onset: rapidDuration: shortMinimum Alveolar Conc:1.3%

    Volatile liquid inhalationanesthetic

    Anesthesia Induction &Maintenance

    Nausea VomitingShiveringMalignant hyperthermia(rare) Elevations inwhite blood countIleus, severe (fatal)Hepatic dysfunction

    Ketamine Ketalar Onset: 30 sec (IV); 3-4min (IM) Duration: 5-10min (IV); 12-25 min (IM):dissociative state maylast >20 min Peakplasma concentration:0.75 pg/mL

    Blocks NMDA receptor Anesthesia Induction Bradycardia DiplopiaHypotensionIncreased IOPInjection-site painNystagmus

    Lorazepam Ativan Onset: 1-3 min (IV insedation); 15-30 min (IMin hypnosis)

    Duration: Up to 8 hr

    Peak plasma time: 2 hr(PO);

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    CNS, including limbicand reticular formation

    Methohexital Brevital Half-Life: 3-6 hrOnset: Immediate (IV); 2-10 min (IM); 5-15 min(PR)Duration: 10-20 min (IV);

    45 min (PR)

    Ultra short-actinganesthetic barbiturate;no muscle relaxantactivity

    Anesthesia Hiccups, coughing,muscle twitching &laryngospasm, whichmay impair pulmonaryventilation

    Midazolam Versed Onset: 15-20 min (IM,PO); 3-5 min (IV)Duration: 1-6 hr (IM)Duration of anterogradeamnesia: 1 hr (IM); 20-40min (IV)Metabolized by liver viaCYP3A4

    Metabolites: 1-hydroxymethylmidazolam

    Binds receptors atseveral sites within theCNS, including thelimbic system andreticular formation;effects may bemediated throughGABA receptor system;increase in neuronalmembrane permeabilityto chloride ionsenhances the inhibitoryeffects of GABA; theshift in chloride ionscauseshyperpolarization (lessexcitability) andstabilization of theneuronal membrane

    Anesthesia HeadacheSedationHiccoughsDeliriumEuphoriaPediatricDesaturationHypotension

    Propofol Diprivan Onset: 30-45 secDuration: 3-10 min (MetabolismMetabolized by hepaticconjugation to inactivecompoundEliminationHalf-life: 40 min (initial);24-72 hr (after 10-day

    infusion)

    Short-acting, lipophilicsedative/hypnotic;causes global CNSdepression,presumably throughagonist actions onGABAa receptors

    AnesthesiaMAC SedationPostoperativeNausea/Vomiting

    Hypotension Apnea lastingMovementInjection siteburning/stinging/pain

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    through intact skin anesthetics stabilizeneuronal membranesand preventgeneration/conductionof nerve impulses

    Flushing Eye/skinirritation N/V DiarrheaChest pain

    Levobupivacaine Chirocaine Parenteral duration 36 h

    Blockade of sodiumchannels

    Longer-durationprocedures

    (but not used topicallyorintravenously)

    Slows, then blocks,action

    potential propagation

    Lidocaine Xylocaine Parenteral (eg,peripheral block, butvaries significantlybased on specificsite) duration 12 h 2 4 h withepinephrine

    Blockade of sodiumchannels

    Short-durationprocedures topical (mucosal),intravenous, infiltration,spinal, epidural, minorand

    major peripheral blocks

    Slows, then blocks,actionpotential propagation

    Mepivacaine Carbocaine Parenteral (eg,peripheral block, butvaries significantlybased on specificsite) duration 12 h 2 4 h withepinephrine

    Blockade of sodiumchannels

    Short-durationprocedures topical (mucosal),intravenous, infiltration,spinal, epidural, minorandmajor peripheral blocks

    Slows, then blocks,actionpotential propagation

    Prilocaine Citanest Parenteral (eg,peripheral block, butvaries significantlybased on specificsite) duration 12 h 2 4 h withepinephrine

    Blockade of sodium

    channels

    Short-durationprocedures topical (mucosal),intravenous, infiltration,spinal, epidural, minorandmajor peripheral blocks

    Slows, then blocks,actionpotential propagation

    Procaine Novocain Parenteral duration30 60 min 60 90 min withepinephrine

    Blockade of sodiumchannels

    Very short procedures(notgenerally used topicallyor

    Slows, then blocks,action

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    CHAPTER 27

    TOPIC : Skeletal Muscle Relaxant

    NAME OF DRUG BRAND NAME PHARMACOKINETIC MECHANISM OF ACTION

    THERAPEUTICINDICATION

    ADVERSE EFFECT

    Atracurium Tracurium Half-Life: Alpha: 2-3.4 minBeta: averages 20 minOnset: 2-2.5 min; maybe slightly delayed inpatients with renalfailureDuration: 20-35 minProtein Bound: 82%

    Non-depolarizingskeletal musclerelaxant; cholinergicreceptor antagonist

    EndotrachealIntubation, MechanicalVentilation

    ErythemaWheezing Increasedbronchial secretionsPruritusUrticaria

    Cisatracurium Nimbex Half-Life, Elim: 22-29minOnset: 2.4-2.6 min(mean for 0.15-0.2mg/kg adult dose)Duration: 55-65 minVd: 145 mL/kg

    Non-depolarizingskeletal musc. relaxant;cholinergic receptorantagonist; a cis-isomerof atracurium

    NeuromuscularBlockade

    Adjunct to generalanesthesia-inducemuscle relaxation forendotrachealintubation, mechanicalventilation

    BronchospasmBradycardiaFlushingHypotensionRash

    Mivacurium Mivacron Onset: Within 60 sec

    Duration: 3-5 min dueto redistribution fromCNS

    Nonbarbituratehypnotic used for theinduction of anesthesia;lacks analgesic activity

    General AnesthesiaInduction

    Transient injection sitepain

    Skeletal musclemovements, mainlymyoclonic

    Opsoclonus Adrenalsuppression

    Pancuronium - Half-Life:2 hr (terminal phase)

    Renal dysfunction may

    Non-depolarizingskeletal musclerelaxant; cholinergic

    General Anesthesia Adjunct/CesareanSection

    Slight elevation in pulserate

    Elevations in blood

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    incr half-life 50% receptor antagonist pressureExcessive salivation

    Rocuronium Zemuron Half-Life1.4-2.4 hr (elimination)

    About 2x as long inhepatic dysfunction

    Nondepolarizingskeletal musclerelaxant; cholinergicreceptor antagonist

    Tracheal Intubation Dose-relatedtachycardia

    Apnea

    Residual muscleweakness

    Succinylcholine Anectine, Quelicin Onset: IV: 30-60 sec;IM: 2-3 min

    Duration: IV 2-10 min;IM 10-30 min

    Depolarizing skeletalmuscle relaxant; noeffect onconsciousness, pain

    Adjunct to generalanesthesia-inducemuscle relaxation forendotrachealintubation, endoscopicexaminations,orthopedic procedures

    Jaw rigidity

    Apnea

    Respiratory depression

    Bradycardia

    Hypotension

    Cardiac arrhythmiasSinus tachycardia

    Vecuronium Norcuron Distribution phase: 3.3-9 min

    Terminal phase: 31-80min

    Non-depolarizingskeletal musclerelaxant; cholinergicreceptor antagonist

    General Anesthesia Hypersensitivityreactions associatedwith histamine release(e.g., bronchospasm,flushing, erythema,acute urticaria,

    hypotension,tachycardia)

    Baclofen Lioresal, Gablofen Onset: 3-4 days

    Duration: 4-8 hr

    Inhibits synaptictransmission throughspinal reflex arcs, viahyperpolarization ofprimary afferent fiberterminals, which mayresult in musclespasticity

    Spasticity Drowsiness, transient

    Dizziness

    Nausea

    Confusion

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    Carisoprodol Soma Onset: 30 min

    Duration: 4-6 hr

    Not clearly known; mayblock interneuralactivity and depresspolysynaptic neurontransmission

    MusculoskeletalConditions

    Dizziness Headache

    Chlorzoxazone - Half-life: 66 min

    Onset: 1 hr

    Duration: 6-12 hr

    Blocks interneuronalconduction in spinal

    cord and subcorticalbrain areas bydepressingpolysynaptic reflexes

    MusculoskeletalConditions

    Dizziness

    Drowsiness

    Excitement,Paradoxical

    Cyclobenzaprine Amrix, Fexmid, Flexeril Hepatic metabolism duration, ~4 6 h

    Poorly understoodinhibition of musclestretch reflexin spinal cord

    Acute spasm due tomuscleinjury inflammation

    Reduction inhyperactivemuscle reflexes antimuscarinic effects

    Dantrolene Dantrium, RevontoPeak plasma time: 5 hr

    Concentration: 100 to>600 ng/mL

    Half-life elimination: 4-8hr

    Duration: 3 hr or longer

    Interferes with calciumrelease within skeletalmuscle cells (fromsarcoplasmic reticulum)

    MalignantHyperthermia (PerMHAUS

    Diarrhea

    Anorexia

    Nausea

    Vomiting

    Gastric irritation

    Diazepam Diastat, Valium Duration: Variable,dependent on dose andfrequency (PO[hypnotic action]); 15-60 min (IV [sedativeaction])

    Modulates postsynapticeffects of GABA-Atransmission, resultingin an increase inpresynaptic inhibition.

    Anxiety Atax

    Euphoria

    Somnolence

    Rash

    Gabapentin Neurontin Bioavailability:Inversely proportion to

    dose; 60% (900

    GABA analogue; Partial Seizure Ataxia DizzinessDrowsiness Fatigue

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    mg/day); 47% (1200mg/day); 34% (2400mg/day); 33% (3600mg/day); 27% (4800mg/day)

    Metaxalone Skelaxin Onset: Within 1 hr

    Duration: 4-6 hr

    Peak plasma time: 3 hr

    General CNSdepression

    Acute PainfulMusculoskeletal

    Conditions

    Nausea

    Vomiting

    Dizziness

    Headache

    Somnolence

    Nervousness

    Methocarbamol Robaxin Hepatic metabolism duration, ~4 6 h

    Poorly understoodinhibition of musclestretch reflexin spinal cord

    Acute spasm due tomuscleinjury inflammation

    Reduction inhyperactivemuscle reflexes antimuscarinic effects

    Orphenadrine Norflex Hepatic metabolism duration, ~4 6 h

    Poorly understoodinhibition of musclestretch reflexin spinal cord

    Acute spasm due tomuscleinjury inflammation

    Reduction inhyperactivemuscle reflexes antimuscarinic effects

    Riluzole Rilutek Half-Life: 12 hr

    Bioavailability: 60%

    Benzathiazole; inhibits

    glutamate release,inactivates voltage-dependent Na+channels, inhibitseffects of excitatoryneurotransmitters

    Amyotrophic Lateral

    Sclerosis (ALS)

    Headache

    Abdominal pain

    Diarrhea DizzinessHypertension

    Tizanidine Zanaflex Bioavailability:40%Peak serum time:1-4 hr

    Alpha-2 adrenergicreceptor agonist

    Muscle Spasticity Dry mouth SomnolenceDizziness Asthenia

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    CHAPTER 36

    TOPIC : Non- steroidal Anti inflammatory drug disease modify antirheumatic Drug, non- opiod Analgesic , Drug use in Gout

    NAME OF DRUG BRAND NAME PHARMACOKINETICS MECHANISM OF

    ACTION

    PHARMACEUTICAL

    INDICATION

    ADVERSE EFFECT

    Acetylsalicylic Acid Easprin Bioavailability: 80-100% Onset: PO, 5-30

    min; PR, 1-2 hr

    Duration: PO, 4-6 hr;

    PR, >7 hr Peak plasma

    time: PO, 0.25-3 hr

    Inhibits synthesis ofprostaglandin by

    cyclooxygenase;

    inhibits platelet

    aggregation; has

    antipyretic and

    analgesic activity

    Pain & Fever AcuteCoronary Syndrome

    Ischemic Stroke &

    Transient Ischemic

    Attack

    AngioedemaBronchospasm CNS

    alteration Dermatologic

    problems

    GI pain, ulceration,

    bleeding Hepatotoxicity

    Hearing loss Nausea

    Platelet aggregationinhibition Premature

    hemolysis

    Bromfenac Xibrom Absorption : Negligible

    systemic absorption

    Half-life: 0.5-4 hr

    Nonsteroidal anti-

    inflammatory agent;

    inhibits COX-1 and

    COX-2, which results in

    decreased formation of

    prostaglandin

    precursors

    Cataract Postoperative

    Ocular

    Inflammation/Pain

    Abnormal sensation in

    eye Conjunctival

    hyperemia Eye irriation

    (burning/stinging) Eye

    pain Eye pruritus Eye

    redness Headache Iritis

    Febuxostat Uloric Absorption

    Bioavailability: 49%

    Peak plasma time: 1-

    1.5 hr Distribution

    Protein bound: 99.2%

    Xanthine oxidase

    inhibitor; inhibits

    conversion of

    hypoxanthine to

    xanthine to uric acid; at

    Chronic Gout Arthralgia Elevated liver

    function test (LFT)

    results Liver function

    abnormalities Nausea

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    Vd: 50 L

    Metabolism

    Metabolized by

    UGT1A1, UGT1A3,

    UGT1A9, and UGT2B7;

    oxidized by CYP1A2,CYP2C8, and CYP2C9;

    also metabolized by

    non-CYP450 enzymes

    Elimination Half-life: 5-8

    hr Excretion: Feces

    (45%; 12%

    unchanged), urine

    (49%; 3% unchanged)

    therapeutic dosages,

    decreases production

    of uric acid without

    disrupting synthesis of

    vital purines and

    pyrimidines

    Rash

    Pegloticase Krystexxa Onset of action: 24 hr

    Duration: 12.5 days

    Half-life: 14 days

    Recombinant,

    pegylated uric acid

    specific enzyme;

    achieves its therapeutic

    effect by catalyzing

    oxidation of uric acid to

    allantoin, therebylowering serum uric

    acid levels

    Gout Gout flares

    Infusion reactions

    Nausea Urticaria

    Probenecid Benamid Half-Life: 3-17 hr

    Onset: 2 hr (effect on

    penicillin levels) Peak

    Plasma Time: 2-4 hr

    Bioavailability: >90%

    (Uricosuric) inhibits

    tubular reabsorption of

    urate; increasing uric

    acid excretion . Also

    inhibits tubular

    Gout, Pelvic

    Inflammatory Disease

    Gonorrhea

    Headache Nausea

    Vomiting Loss of

    appetite GI upset Rash

    Flushing Dizziness

    Fever Aplastic anemia

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    Protein Bound: 85-95%

    (albumin) Metabolism:

    Liver Metabolites:

    hydroxylated

    metabolites, N-

    despropyl metabolite,

    probenecid

    acylglucuronide

    Excretion: Urine

    secretion of weak

    organic acids like PCNs

    & cephalosporins

    Hemolytic anemia

    Leukopenia

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