lOMoARcPSD|4019340

Pharmacology Notes for Board Exam Reviewer

Physical Pharmacy (Our Lady of Fatima University)

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Pharmacology
Study of substances that interact with living DRUG TARGET SITES
systems through chemical processes by binding
to regulatory molecules and activate in or Structural Protein
inhibiting normal body processes. Constitute “Cytoskeleton”

Drug ______________________- important site of action

It is any substance that brings about change in Drugs that inhibit microtubule synthesis
biological function through its chemical Spindle protein
actions. Griseofulvin
Use for the: Vinca alkaloids
1. Prevention – to prevent or hinder the Colchicine
occurrence of disease (e.g. MMR Vaccine, Etoposide
Vitamin A)
2. Diagnosis – to determine the presence or Regulatory Proteins
absence of disease (e.g Barium Sulfate, Mediates the transmission of endogenous
Edrophonium) chemical signals such as neurotransmitters,
3. Mitigation – to stop progression of disease autacoids or hormones
(e.g. anti-parkinsons drugs, captopril) Transport Channels
4. Treatment – to manage symptoms of Enzymes
disease (e.g. antibiotic, analgesic) Carrier Molecules
5. Cure- the total recovery or relief from Receptors
disease
__________________________________
Voltage Gated Na- Channel
Inhibitors
Na Channel Blocker
Local Anesthetics
Carbamazepine
Phenytoin
Tetrodotoxin
Voltage Gated Ca- Channel
Calcium channel blockers “dipines”

____________________________________
Na- K ATPase Pump – Digoxin
H – K ATPase Pump – PPI
Na- K- 2 Cl Transport – Furosemide
Na – Cl – transporter – Thiazides

_____________________________
Acetylcholinesterase - Edrophonium
COMT – Entacapone

_________________________
Functional macromolecular components of
cells with specific stereo chemical
configuration and in which ligand interacts
PHARMACODYNAMICS

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

*____________________ – any chemical that has Partial - ________________________

ability to bind to a receptor

Type I Antagonist
______________________________ _______________________ – with affinity but no
Found in cell. Ligand membrane receptors intrinsic activity
stimulated in nicotinic milliseconds receptor a. Pharmacodynamic antagonist – same
receptor (e.g. Propranolol + Epinephrine)
Type II b. Pharmacokinetic antagonist – reduce
_____________________________________________________ the effect of one drug by alteration of time
___________________________________________________ (e.g. Digoxin + Cholestyramine)
Located in the cell membrane receptors
______________________ - different receptor sites
Type III (e.g. Histamine + Epinephrine; Glucocorticoid +
_____________________________ Insulin)
Located in nucleus. Receptor for insulin
utilization of glucose. _______________________ - it prevents the binding
Onset: hours of agonist, no receptor is involved
(e.g. Protamine sulfate + Heparin Sulfate;
Type IV Paracetamol + N- Acetyl cysteine; Warfarin +
_____________________________ Vitamin K)
Located in steroid nucleus/ Vit D cytosol.
Onset: hours NATURE OF ANTAGONISM

Theories of Drug Receptors Interaction Competitive antagonist- Effects of Antagonist

Occupancy Theory can be overcome/reversed by increasing the
Drug effects is directly proportional to the concentration of agonist
number of receptors occupied
NON-COMPETITIVE ANTAGONISM
Lock and Key Mechanism it is also known as irreversible antagonism

Induced Fit Theory

ENHANCEMENT OF DRUG EFFECTS
Ariens / Stephenson Theory
Occupational theory of response 1. ADDITION
 A drug effect that is equal in the
Rate Theory magnitude
The activation of receptor is directly to the sum of the individual effects of two
proportional to the total number of drugs.
encounters of drug with its receptor per unit  Two different drugs with the same
time effect are
given together.
Classification of Drugs According to
Receptor Interaction 2. SYNERGISM
Agonist  The effect of two drugs is greater in
Drug that binds to same binding site as an magnitude than the sum of the
agonist for that receptor or reverses constitute individual effects of the two drugs.
activity of receptors  Two drugs with same effect are given
together.
Full – ___________________________

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

3. POTENTIATION Rece
Post
 Occurs when one drug, lacking an ptor Distribution Mechanism
Receptor
effect of its own, increases the effect of Type
another drug that is active. Vasodilatio
Smooth
 1+0=2 n, increase
muscle ↑Ip3,
 Tyramine-containing Foods + MAOI H1 in
endothelium, DAG (Gq)
permeabili
Brain
ty
Autacoids ↑ cAMP
“Autos” (self) and “acos” (relief, drug) Gastric
(Gs)
Aka “Local Hormones” mucosa, Increase
stimulati
Localized effect: Self Release H2 cardiac release of
on of
muscle, mast HCL
adenyl
5 classes: cells, brain
cyclase
1. Biologically active amine Myenteric
Decreased
Serotonin and histamine plexus, ↓ cAMP,
H3 Ach
presynaptic Ca (Gi)
Release
2. Lipid derived autacoids (Eicosanoids) brain
Prostaglandins Eosinophils,
↓cAMP,
Leukotrienes H4 Neutrophils,
Thromboxanes Ca (Gi)
CD4 T-cells

3. Ergot Alkaloids
Histamine Agonist
4. Vasoactive Polypeptides _____________________________ – used in allergy
Angiotensin testing
Endothelin _____________________________ – used to test of
Kinins gastric secretory function
Natriuretic Peptide Impromidine
Substance P
Vasopressin Histamine (H1) receptor antagonist
Aka: Antihistamine
5. Endothelium-derived Autacoids Competitive inhibitor at the H1 receptor
Nitric Oxide
Anti-Histamines
Biologically active amines 1st Gen
Histamine ______________________________
Precursor: Histamine Carbonoxamine
Process: Decarboxylation Dimenhydrinate
Storage: Mast Cells Diphenhydramine
Doxylamine
Process: _____________________________
1. Energy and Ca-dependent Degranulation Pyrilamine
reaction (Immunologic release) Tripelenamine
2. Energy and Ca-independent release ____________________________
(Displacement) Hydroxyzine
Meclizine
Types of Histamine Receptors: ___________________________
Brompheniramine

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Chlorpheniramine C. metabolized in the liver;

___________________________  many induce microsomal enzymes
Promethazine and alter their own metabolism
Miscellaneous:
Cyproheptadine ADVERSE EFFECTS
o sedation (synergistic w/ alcohol,
2nd Gen other depressants, dizziness, and loss of
Adv: less sedating effect and less frequency of appetite.
administration o gastrointestinal upset, nausea,
constipation and diarrhea.
Piperidines: o anticholinergic effects (dry mouth,
Fexofenadine blurred vision, and urine retention).
Ferfenadine
Astanizole H2 receptor antagonist
Miscellaneous: Used in the treatment of gastrointestinal
Loratidine disorders, heart burn or acid induced
Cetirizine indigestion, promote the healing of gastric or
duodenal ulcers, hypersecretory states such as
Uses: Zollinger Ellison Syndrome
o Treatment of allergic rhinitis and
conjunctivitis. _____________________ (Tagamet) – Anti
 treat the common cold based on their androgenic activity; potent enzyme inhibitor
anticholinergic properties _____________________ – 100% Bioavailable
 Diphenhydramine also has an Famotidine
antitussive effect not
mediated by H1-receptor Cimetidine, ranitidine, and famotidine
antagonism.  undergo first-pass hepatic metabolism
 Treatment of urticaria and atopic resulting in a bioavailability of
dermatitis, including hives approximately 50%.
 Sedatives  Nizatidine has little first-pass
 Several (doxylamine, metabolism and a bioavailability of
diphenhydramine) are almost 100%.
marketed as over-the-counter
(OTC) sleep aids. Inhibitors of histamine release
 Prevention of motion sickness Mast cell stabilizers:
 Appetite suppressants Cromolyn (Intal)
Nedocromil Sodium (Tilade)
Pharmacokinetic Properties of H1
Blocking Drugs Inhibitors of Histamine release
1. Poorly absorbs salts
A. well absorbed after oral administration. 2. Inhibit release of histamine or other
o Normal effects seen in 30 minutes autacoids from the mast cells
(with maximal effects at 1-2 hours) 3. Prophylactic agent in asthma
o The duration of action is : 4. Nedocromil Sodium – appears to be more
 1ST generation compounds: 3-6 effective in reducing bronchospasm
hours caused by exercise or cold air
 2ND generation compounds: 3-24 5. ADR: Sore throat/ dry mouth
hours
B. lipid-soluble = cross the blood-brain barrier

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

GIT these receptors mediate an increase in

Serotonin = 5-HT (5- hydroxytryptamine) secretion or peristalsis
Serotonin in muscles – contraction
An indole amine has an indole ring structure
This structure is also “hallucinogenic” or SEROTONIN AGONISTS
psychedelic drugs Buspirone (Buspar)
Sumatriptan (Imitrex)
Serotonergic systems Trazodone (Desyrel)
Plays important role in sleep, elevated mood, Cisapride (Propulsid)
decreased appetite, increase temperature Tegaserod
regulation, pain perception
* Serotonin – melatonin (sleep hormone) (indirect agonist)
through pineal gland. Fluoxetine
Dexfenfluramine
Serotonin synthesis Sibutramine
Undergo decarboxylation
Tryptophan → Tryptophan hydroxylase → Serotonin Antagonists
5-HTP → 5-HTP decarboxylase 1. Cyproheptadine (Periactin)
→5HT 2. “Setron” - Ondansetron,
Granisetron (Kytril)
Tissue Distribution 3. Ketanserin Ketanserin (Sufrexal)
_______________________ of GI tract (90%) 4. Clozapine (Clozaril)
Platelets (10%) 5. Risperidone (Risperdal)

Metabolism
Phase I
Serotonin → (MAO) → 5-hydroxyindole Ergot – from Claviceps Purpurea
acetaldehyde → (Acetaldehyde Powerful hallucinogen
dehydrogenase) → ______________________________ Affects the following receptors:
 Adrenoceptors
 Dopamine receptors
5HT1  Serotonin receptors
Contract arterial esp in carotid smooth muscle
Ergotism
5HT2 Accidental ingestion of ergot alkaloids in
Platelet “causes aggregation” contaminated grain
Most dramatic effects of poisoning are:
CNS – mediated hallucinogenic effects Dementia with hallucinations, prolonged
Contraction of vascular smooth muscle vasospasm, gangrene, stimulation of uterine
smooth muscles
5HT3 “St. Anthony’s Fire”
Stimulation of receptor in area postrema
Causes nausea and vomiting Effects:
Peripheral sensory or neurons causes pain or Vascular smooth muscle = Contraction
afferent vagal nerve – chemoreceptor reflex Uterus = contraction
Also known as Bezold Harish reflex Endocrine = suppress prolactin secretion from
Bradycardia/ hypotension pituitary cells

5HT4 USES:
I. Migraine

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

1. Ergotamine,
Cafergot (caffeine and ergotamine] USES:
2. Methysergide Female Reproductive System
Its therapeutic effect in migraine prophylaxis a. Abortion:
has been associated with its antagonism at  Dinoprostone (PGE2)
the 5-HT2B receptor a synthetic preparation administered
It has a known side effect, retroperitoneal vaginally for oxytocic use.
fibrosis, which is severe, although uncommon.  Carboprost Tromethamine (15-
methyl-PGF2a)
II. Post-partum hemorrhage administered as a single 2.5 mg intra-
 Ergonovine maleate amniotic injection.
This medication is used after childbirth to help  Antiprogestins (Mifepristone)
stop bleeding after delivery of the combined with an oral oxytocic
placenta (afterbirth). prostaglandin (Misoprostol) to
produce early abortion.
III. Hyperprolactinemia
- the presence of abnormally high Male Reproductive System
levels of prolactin in the blood Erectile Dysfunction – Alprostadil (PGE1)
o Prolactin (PRL), also known as need vasodilator
lactotrope, is a protein that in
humans is probably best Pulmonary Hypertension
known for its role in PGI2 lowers peripheral pulmonary or coronary
enabling female mammals resistance Prostaglandin (PGI2,
to produce milk Epoprosterol, Iloprost)

Bromocriptine Peripheral Vascular Disease

 Bromocriptine (INN; trade names PGE & PGI2
Parlodel, Cycloset), an ergoline
derivative, Patent ductus arteriosus
 is a dopamine agonist that is used in Alprostadil (PGE1)
the treatment of pituitary tumors,
Parkinson's disease, Blood
hyperprolactinaemia, neuroleptic Platelet aggregation: TXA2
malignant syndrome
Pergolide
 is an ergoline-based dopamine Gastrointestinal System
receptor agonist used in some Misoprostol (PGE1)
countries for the treatment of Available in Europe/ USA
Parkinson's disease. DOC for NSAID induced ulcer

Eicosanoids Glaucoma
Derived from lipids Latanoprost – a tablet; long acting PGF 2a
Large group of autacoids with potent effects on Bimatoprost
virtually every tissue in body Tavaprost
Derived from metabolism of 20-carbon, Unoprostone
unsaturated form (Arachidonic)

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

PG ANTAGONISTS

NSAIDs
Drug Classes: Examples
propionic acid derivative ibuprofen
pyrrolealkanoic acid derivative tolmetin
phenylalkanoic acid derivative flubiprofen
indole derivative indomethacin
pyrazolone derivative phenylbutazone
phenylacetic acid derivative diclofenac
Fenamate mefenamic
Oxicam piroxicam PERIPHERAL NERVES
naphthylacetic acid prodrug nabumetone -collection of nerves and ganglia scattered
throughout the brain
-consist of 12 pairs of cranial nerves, 31 pairs
of spinal nerve and their branches to the entire
Inhibition of COX prostaglandin
body
Common ADR: GI irritation or upset
Ex. Aspirin – inhibition of TXA2 – anti-
CRANIAL NERVES:
inflammatory activity
I. OLFACTORY NERVE
COX-2 Inhibitor- “Coxib” II. OPTIC NERVE
Celecoxib, Valdecoxib, Enterocoxib III. OCCULOMOTR NERVE
IV. TROCHLEAR NERVE
Lipooxygenase Pathway Produces: V. TRIGEMINAL NERVE
VI. ABDUCNES NERVE
VII. FACIAL NERVE
Leukotrienes VIII. AUDITORY OR VESTIBULOCOCHLEAR
NERVE
Leukotriene Receptor inhibitors IX. GLOSSOPHARYNGEAL NERVE
X. VAGUS NERVE
Leukotriene antagonists are used to treat these
XI. SPINAL ACCESSORY NERVE
disorders by inhibiting the production or
XII. HYPOGLOSSAL NERVE
activity of leukotrienes

Respiratory System
 Leukotriene Receptor Inhibitors
(Zafirlukast, Montelukast)
 5-Lipoxygenase Inhibitor
(Zileuton)

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Major Subdivision of PNS Adrenergic Drugs

1. Autonomic - stimulate the sympathetic NS
2. Somatic - adrenergic agonist, sympathomimetic and
3. Enteric NS adrenomimetic
-they mimic norepinephrine and epinephrine
Enteric Nervous System- include the -act on one or more receptor sites
myenteric plexus (plexus of auerbach) and
submucous plexus (plexus of meissner) Classification of Sympathomimetic/ Adrenergic
Drugs according to their effect
Somatic Nervous System- concerned with DIRECT ACTING- stimulates the adrenergic
consciously controlled functions such as receptors
movement, respiration and posture
INDIRECT ACTING- stimulate the release of NE
Autonomic Nervous System- autonomous from the terminal nerve ending amphetamine
(independent)
-concerned primarily with visceral functions, MIXED ACTING- both-ephedrine
cardiac output, blood flow to organ, it’s
activities are not under direct conscious MIXED ALHPA AND BETA AGONIST
control
•EPINEPHRINE
2 DIVISIONS: (beta 2) -rapidly acting bronchodilator
1. Sympathetic NS (alpha 1)- used to prolong the acitivity of local
2. Parasympathetic anesthetic
(beta 1)- used to restore the cardiac activity in
(Please utilize the space at the back) cardiac arrest
(alpha 1)-topically treatment of glaucoma
(2% solution )
Sympathetic NS
•NOREPINEPHRINE
5 Steps of Neurotransmission (Levarterenol, Noradrenaline)
1. Synthesis
2. Storage ALPHA AGONIST
3. Release Methoxamine- for hypertension (parenteral)
•Bretylium
•Guanethidine Midodrine- used in the treatment of postural
4. Receptor Binding hypertension
5. Reuptake/Removal -prodrug that is hydrolyzed is
•Cocaine desglymidodrine
•TCA

Removal of Norepinephrine
1. Diffusion B. DECONGESTANTS
2. Metabolism B.1 Phenylephrine
-enzymes that inactivate NE - has longer duration of action than the
•MAO (Monoamine Oxidase Enzymes) catecholamine
•COMT (Catechol o-methyl transferase) -mydriatic and decongestant
Metabolites- are extracted in the urine *REBOUND CONGESTION- rhinitis
3. Reuptake- recaptured by an uptake system medicamentosa
-pulls the NE back to neuron B.2 Phenylpropanolamine

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

B.3 Xylometazoline and Oxymetazoline

OTHER SYMPATHOMIMEMTIC
Ephedrine
ALPHA 2 AGONIST
• Clonidine CNS stimulants
• Methyldopa Amphetamine
• Guanfacine Methylphenidate/Pemoline for ADHD
• Guanabenz Use: narcolepsy- uncontrollable state
Use in the treatment of hypertension
MOA: inhibit the release of NE from *Tyramine -normal by product of tyrosine
sympathetic nerve endings metabolism metabolized by MAO
-inactive when taken orally
BETA AGONIST because of a very high 1st pass effect
Isoproterenol (Isoprenaline)
B1 = B2 >>> a CATECHOLAMINE REUPTAKE INHIBITORS
Atomoxetine - for ADHD
Effects: Reboxetine - for ADHD
positive chronotropic/ inotropic actions Duloxetine - antidepressant
bronchodilation Milnacipran - fibromyalgia
peripheral vasodilation Sibutramine – anti-obesity agent
Cocaine -CNS stimulant/LA
BETA 2 AGONIST
Anti-asthma drugs:
Albuterol ALPHA BLOCKERS – vasodilating
Terbutaline effect into the blood vessels
Metaproterenol
Salmeterol NONSELECTIVE ALPHA BLOCKING AGENTS
Phentolamine (reversible)
Tocolytic drugs:
Phenoxylamine (irreversible)
Ritodrine
Uses: pheochromocytoma
Terbutaline
erectile dysfunction
relieve vasospasm Reynaud’s syndrome
BETA 1 SELECTIVE AGONIST
Dobutamine
SELECTIVE APLHA 1- AGONIST
“Zosins”
Major limitations:
• Terazosin
• Tolerance- prolong use
• Doxazosin
• Chronic cardiac stimulation in patient
• Alfusozin
w/ heart failure may worsen long term
outcome
Tamsulosin- oral route, increase IFIS
(Intraoperative Floppy Iris Syndrome) for
DOPAMINE 1 AGONIST
patients undergoing cataract surgery
Fenoldopam -for treatment of severe HTN Alfuzosin- risk: QT prolongation
Silodosin- for BPH
DOPAMINE AGONIST Indoramin- antihypertensive
Dopamine -the immediate metabolic precursor Urapidil- antihypertensive/BPH
of norepinephrine
-activates D1 receptor several Adverse effects: 1st dose phenomenon
vascular beds which leads to vasodilator “syncope”

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

-adjust the dose to 1/3 or ¼ of normal • Bronchoconstriction

dose • Arrhythmias
-admin a bedtime • Sexual impairment
• Disturbance in metabolism
Orthostatic hypotension
*Nadolol- with long duration of action
*Esmolol- ultra short acting beta blocker
ALPHA 2 BLOCKERS
Yohimbine –erectile dysfunction CARDIOSLECTIVE BETA BLOCKERS
Rauwolscine B-1 BLOCKERS
Tolazoline •Bisoprolol
•Esmolol
NON SELECTIVE BETA BLOCKERS •Atenolol
*Propranolol- prototype agent •Nevibolol – most highly selective beta blocker
Carteolol •Acebutolol
Nadolol •Metoprolol
Penbutolol •Celiprolol
Pindolol
Sotalol With ISA (Intrinsic Sympathomimetic Activity)-
partial agonist effect
Propranolol • Pindolol (Visken)
Actions: • Acebutolol (Sectral)
-Cardiovascular • Labetalol (Trandate)
• Decrease cardiac output, (-) inotropic/ Advantage: less associated w/rebound HTN or
chronotropic tachycardia upon withdrawal
• Oxygen consumption decrease –used in
angina With MSA (Membrane Stabilizing Activity)-
• Decrease cardiac output and blood anesthetic effect
pressure • Pindolol
 Bronchoconstriction • Acebutolol
□ Due to blockade of Beta2 • Labetalol
□ Can ppt reapiratory crisis in patient • Propranolol
with COPD and asthma • Metoprolol
• Decrease BP Disadvantage: cannot be given as ocular topic
 Disturbance in glucose metabolism agents
o Beta blocker –decrease glycogenolysis
 Blocks action of Isoproterenol MIXED ALPHA/ BLOCKERS
•Labetalol (Trandate)
Uses: -alternative to hydralazine in treatment of
• Prophylaxis of angina pectoris, pregnancy induced hypertension
supraventricular and ventricular dysrhythmias •Carvedilol (Coreg)
• Migraine headache -CHF
• Anti-hypertensive
• Negative chronotropic agent in anxiety BETA BLOCKERS USED IN GLAUCOMA
(stage fright and hyperthyroidism) Non selective:
• For chronic glaucoma •Timolol
• For MI •Levobunol
Selective Beta 1 Blocker
ADR’s: •Betaxolol

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Partial Agonist - Nicotine

•Carteolol - Muscarine
Others: Metipranol
*BETANECHOL- for management of ileus and
CHOLINERGIC AGONISTS & ANTAGONISTS urinary retention
*CARBACHOL CHLORIDE AND PILOCARPINE-
for glaucoma

*INDIRECT ACTING- inhibit the action n of

enzymes acetylcholinesterase

•Edrophonium -reversible, short acting,

diagnostic agent
•Carbamates -reversible, suffix “tigmine”,
intermediate acting
•Organophosphate -irreversible, suffix “phate”,
long acting

DRUGS AFFECTING NEUROTRANSMITTER Treatment of organophosphate poisoning

STORAGE 1. REGENERATOR COMPUNDS
Reserpine - plant alkaloid -used in early in the course of poisoning
Botolinum Toxin -facilitate removal of binding of
____________________ organophosphate
-oxime derivatives (PRALIDOXIME)
INACTIVATION OF ACETYLCHOLINE 2. PHYSIOLOGIC ANTIDOTE
1. Acetylcholinesterase -Atropine-long term administration is needed
2. Butyrylcholinesterase

DRUGS CHOLINERGIC ANTAGONISTS

 Red as a beet
*DIRECT ACTING – directly stimulating the  Hot as hell
cholinergic receptors  Dry as a bone
*INDIRECT ACTING - ____________________________  Blind as bat
____________________________________________________  Mad as hatter

DIRECT ACTING CHOLINOMIMETIC Atropine

1. ESTERS OF CHOLINE OR CHOLINE Pirenzepine
ESTERS Trihexyphenidyl
- acetylcholine Ipratropium
- betanechol Glycopyrrolate
- metacholine chloride Scopolamine (methyl derivative)
- carbachol chloride

2. ALKALOIDS
- Pilocarpine

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

ATROPINE
- prototype NICOTINIC BLOCKING AGENT
SOURCES: According to the nicotinic receptors they block
 Atropa belladonna 1. Ganglionic blockers- inhibit NN
▪ or deadly nightshade 2. Neuromuscular blockers- inhibit NM
 Datura stramonium
▪ also known as GANGLIONIC BLOCKERS
jimsonweed 1. Tetraethylamonium (TEA)
(Jamestown weed) or 2. Hexamethonium (“C6”)
thornapple. 3. Decamethonium (“C10”)

SCOPOLAMINE MECAMYLAMINE- a secondary amine, was

 - aka hyoscine developed to improve the degree and extent of
 - alkaloid from henbane (Hyoscyamus absorption from the GIT
niger)
 - prevent motion sickness- TRIMETHAPHAN- a short acting ganglion
transdermal patch blocker, is inactive orally and given by IV
 -S/E: constipation, urinary retention… infusion

HOMATROPINE
 (Isopto Homatropine), Cyclopentolate INTRODUCTION TO CNS PHARMACOLOGY
(Cyclogyl), Tropicamide (Mydriacyl)
 - ophthalmoscopic examination Ion Channels and
Neurotransmitter Receptors
IPRATROPIUM
 quaternary amine- more peripheral ION CHANNELS
effect (lungs), Voltage- Causes influx
 less CNS effects Regulatory
gated of ions
 - asthma Ligand-gated
Pirenzepine
NEUROTRANSMITTER RECEPTORS
 - peptic ulcer
Ionotropic Type
receptors I
Benztropine (Cogentin), Trihexyphenidyl
Membrane-
(Artane), Biperiden (Akineton)
Metabotropic Type delimited
 - Parkinson’s disease
receptors II Diffusible second
messenger
Gastrointestinal Disorders
 Peptic ulcer (rarely used
nowadays)
▪ Propantheline,
glycopyrrolate,
clinidium SYNAPTIC POTENTIALS
 Relieve traveller’s diarrhea and Excitatory Post- Inhibitory Post-
other mild or self limited Synaptic Synaptic
hypermotility Potentials (EPSP) Potentials (IPSP)
 Atropine + Diphenoxylate Depolarization Hyperpolarization
(Lomotil) ↑ Neuronal Activity ↓ Neuronal Activity
Activation below Depression
CHOLINERGIC POISONING the threshold (-

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

60mV) 2. Barbiturates
3. Other drugs
CNS DRUGS • Ethanol, chloral hydrate
• CNS depressant • Zolpidem
• Sedative hypnotic • Zaleplon
• Anti-psychotic • Eszopiclone
• General anesthetics • Ramelteon
• Narcotic analgesic • Buspirone

SEDATIVE HYPNOTIC -CALMING EFFECT AND BENZODIAZEPINE

SLEEP • Chlordiazepoxide (Librium)
• Diazepam (Valium)
Anxiety • Temazepam (Restoril)
 refers to many states in which the • Triazolam (Halcion)
 sufferer experiences a sense of • Clonazepam (Klonopin)
impending threat or doom that is not • Lorazepam (Ativan)
well defined or realistically based. • Alprazolam (Xanax)
 usually accompanied by symptoms • Flunitrazepam (Rohypnol)
such as tachycardia, palpitations,
tachypnea, sweating, trembling and 1. Short-acting (2-8 hrs)
weakness  Oxazepam (Serax)
Types:  Triazolam (Halcion)
1. Panic disorder- recurrent unexpected  Clonazepam (Klonopin, Rivotril)
panic attacks that can occur with agoraphobia  Midazolam (Versed, Dormicum)
in which patients fear places in which escape 2. Intermediate-acting (10-20 hrs)
might be difficult.  Lorazepam (Ativan)
 Alprazolam (Xanax, Xanor)
2. Specific phobia- intense fear of particular  Temazepam (Restoril)
objects or situations (e.g. snakes, heights); 3. Long-acting (1-3 days)
most common psychiatric disorder  Diazepam (Valium, Anxionil)
 Flurazepam (Dalmane)
3. Social phobia- intense fear of being  Chlordiazepoxide (Librium)
scrutinized in social or public situations (e.g.,
giving a speech, speaking in class). USES:
 Anxiety- alprazolam, diazepam
4. Generalized anxiety disorder- intense  Seizures- diazepam, clonazepam,
pervasive worry over virtually every aspect of lorazepam
life  Insomnia- flurazepam, midazolam
5.Post-traumatic stress disorder- persistent  Pre-operative sedation- midazolam
re-experience of a trauma, efforts to avoid
recollecting the trauma, and hyperarousal S/E:
 drowsiness, dependence
6. Obsessive-compulsive disorder-  respiratory depression (+ ethanol,
recurrent obsessions and compulsions that other CNS depressants)
cause significant distress and occupy a  Antidote: Flumazenil (Anexate)- GABA
significant portion of one’s life receptor antagonist

Benzodiazepine MOA: bind to GABA; increase

DRUG CLASSIFICATIONS: frequency of Cl channel opening enhancing
1. Benzodiazepine membrane hyperpolarization.

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

 Buspirone binds to 5-HT type 1A

DRUGS FOR THE TREATMENT OF serotonin receptors
WITHDRAWAL SYMPTOMS  It also possesses both dopamine
•Diazepam agonist and indirect dopamine
•Clonazepam antagonist properties.
•Phenobarbital –for mixed bzd and alcohol  Doc for chronic persistent anxiety
dependence

BARBITURATES  RAMELTEON (ROZEREM)

• Amobarbital (Amytal)  Melatonin Receptor Agonist
• Pentobarbital (Nembutal)  MOA: Activates MT1 and MT2
• Phenobarbita (Luminal) receptors in suprachiasmatic
• Secobarbital (Seconal) nuclei in the CNS
 Rapid onset of effect with
 former DOC for anxiety, insomnia minimal rebound insomnia
 barbituric acid is 2,4,6
trioxohexahydropyrimidine
 Propranolol and other beta-
MOA: Barbiturates increase the duration of blockers may be useful in patients
GABA-mediated chloride ion channel opening with prominent cardiovascular
symptoms of anxiety.
1. Ultra-short (20 min):  They are less effective
 Thiopental (Pentothal) anxiolytics than BZs, and
2. Short-acting (3-8 h): their usefulness may be
 Pentobarbital (Nembutal) restricted to those anxiety
 Amobarbital (Amytal) patients with physical
3. Long-acting (1-2 d): symptoms, especially
 phenobarbital (Luminal) cardiovascular complaints,
4. Intermediate-acting: have not adequately responded
 amobarbital, butabarbital to BZ therapy.

USES: *CHLORAL HYDRATE

 induction of anesthesia- Thiopental - associated to Mickey Finn
 seizures in children- Phenobarbital *TRICHLOROETHANOL- active metabolite
 anxiety- Pentobarbital, Amobarbital *TRICHLOROACETIC ACID-toxic metabolite

NEWER HYPNOTICS
•Eszopiclone (Lunesta)
Psychosis
-cyclopyrrolone Denotes a variety of mental disorders
•Zaleplon (Sonata)
-pyrazolopyrimidine Schizophrenia
•Zolpidem (Ambien) Clear sensorium but marked thinking
-imidazopyrimidine disturbances.

Course of Schizophrenia
BUSPIRONE •Prodromal
 serotonin agonist •Active
 non-sedating, no dependence •Residual

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Symptoms: Management
 Characteristic symptoms: •Psychosocial therapy
 Two or more of the following, each •Institutional approaches
persisting for a significant portion of at •Cognitive-behavioral therapy
least a 1-month period: •Family communication and education
▪ Positive symptoms
▪ Disorganized speech Treatment
▪ Grossly disorganized or -Anti-psychotics
catatonic behavior -neuroleptics/ major tranquilizers
▪ Negative symptoms
History
Reserpine and chlorpromazine – 1st drug
Positive Symptoms of Schizophrenia used
•Hallucination and delusion
Clinical use of anti-psychotic
A. Psychiatric Indication
• Schizophrenia
• Schizoaffective disorder
• Bipolar affective disorder
• Tourette’s syndrome
• Senile dementia of Alzheimer type
B. Neuropsychiatric indication
• Antiemetic
• Antihistamine
• Preoperative sedatives
Negative symptoms • Neurolept-anesthesia
•Flat effect
•Alogia MOA of Neuroleptics
•Avolition •Typical block the postsynaptic Dopa receptors
•Asociality •Atypical block serotonin receptors
•Anhedonia
•Incoherence Typical Anti-Psychotics
•Loose associations •Phenothiazine (aliphatic, piperidine and
piperazine)
Others: •Butyrophenone
•Catatonia •Thioxanthine
•Catatonic immobility
•Waxy flexibility
•Inappropriate effect Atypical
•Clozapine
Pathophysiology
•Risperidone
-Neurotransmitter changes •Olanzapine
•Serotonin, dopamine and glutamine •Sertindole
•Dibenzoxapine
•Dibenzodiazepine
Risk of Schizophrenia •Benzisoxazole
•Predisponsing factors •Thiobendazole
•Precipitating factors •Fluorophenylyindole
•Quetiapine

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

•Sulpride and sulpiride

Summary of side effects

•Monoamine hypothesis

•Neuro endocrine factors

Therapy of depression
•Non pharmacological
•Pharmacological

Treatment Phase
•Acute
Affective Disorders •Continuation
-mental illness characterized by pathological •Maintenance
changes in mood.
Pharmacotherapy
(unipolar and bipolar) •SSRI
•TCA
Major Depressive Disorder •MAOI
-depressed mood most of the time •ATYPICAL ANTIDEPRESSANT
•SARI
Symptoms •SNRI
•Feeling of guilt •NDRI
•Disturbed sleep and appetite •NaRI
•Low energy •NaSSA
•Poor concentration
•Suicidal attempts Selective Serotonin Reuptake Inhibitors
• Fluoxetine
Medical Condition • Sertraline
•Chronic pain • Citalopram
•Coronary artery disease • Escitalopram
•Diabetes • Paroxetine
•Stroke • Fluvoxamine
Pathophysiology Tricyclic Anti-Depressant
•Neurotropic Hypothesis
• Imipramine
• Amitriptyline
• Nortriptyline

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

• Desipramine 5T2A Reuptake Inhibitors

• Doxepin • Trazodone
• Amoxapine • Nefazodone
• Maprotiline
Tetracyclic and Unicyclic anti depressant
Indication: • Bupropion
• Severer major depression • Mirtazapine
• Panic disorder • Amoxapine
• Enuresis • Maprotiline

Bipolar Disorder
Adverse Effect -imbalance of neurotransmitter
• Anti cholinergic manifestation
• Cardiac overstimulation Diagnosis of Bipolar is made using the DSM-IV-
• Orthostatic hypotension TR criteria and reviewing the individual
• Sedation history for episodes of mania hypomania and
depression.
Selective serotonin – NE reuptake inhibitor
Drugs Symptoms of Mania
• Venlafaxine • Grandiose ideation
• Desvenlafaxine • Decrease need of sleep
• Duloxetine • Pressured speech
• Racing thoughts or ideas
Characteristics
• Like TCA Bipolar Disorder
• Improved profile in AE Effects Category
• Very effective • Bipolar 1 disorder
• Bipolar 2 disorder
Adverse Effect • Cyclothymia
• Nausea • Bipolar N.O.S
• Vertigo
• HTN Pharmacotherapy
• Manic reaction -depend on clinical presentation.

Monoamine Oxidase Inhibitor Short term treatment for mania

• Phenelzine • Olanzapine
• Isocarboxasid • Haloperidol
• Trancyloprine • Benzodiazepines
MOA • Bupropion or paroxetine
-Inhibition of intracellular MAO in the CNS
Indication: Lithium – used prophylactically in treating
-for patient unresponsive in TCA manic depressive patients and in the treatment
Patient with low psychomotor of manic episodes

Adverse effect Adverse effect of Lithium

• Drowsiness • Ataxia
• Orthostatic hypotension • Tremors
• Blurred vision • Confusion
• convulsion

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Disorder characterized by a variety of

abnormal movements

Movement disorders Wilson’s disease

Basal ganglia- responsible for initiating, Copper poisoning
sequencing, and modulating motor activity. Treatment:
Penicillamine
Different types of abnormal movement Trientine
Tetrathiomolybdate
Tremor Zinc acetate
-postural/essential tremor Zinc sulfate

Drug for essential tremor Parkinson’s disease

Propranolol Paralysis agitans
Metoprolol Dr. James Parkinson- “shaking palsy”
Primidone Neurodegenerative disease associated with
Topiramate depigmentation of substantia nigra
Alprazolam Characterized by distinctive motor disability
Gabapentin
-intention tremor Forms

Chorea Primary (idiopathic) parkinsonism

Involuntary, unpredictable muscle jerks that Unknown cause
occur in different parts of the body and impair Classic
voluntary activity. Dance like Treatment may be palliative

Ballismus Secondary parkinsonism

Violent flinging movement Identifiable cause
Caused by drugs- dopamine antagonists, such
Huntington’s disease as:
Characterized by progressive chorea and Phenothiazines
dementia Butyrophenones
Reserpine
Athetosis Poisoning by chemical or toxins
Infectious disease
Abnormal movements may be slow and
writhing in character
Symptom of Parkinson’s disease
Tremor
Dsytonia
Rigidity
Sustained abnormal postures Akinesia
Postural instability
Tics
Sudden uncoordinated abnormal movements Classification of drug therapy for Parkinson’s
that tend to occur repetitively. disease
Dopaminergic agents
Gilles de la Tourette’s syndrome Promote activation of dopamine receptors
Chronic multiple tics Anticholinergic agents
Prevent activation of cholinergic receptors
Tardive dyskinesia
Mechanism of action

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

5. Blockade of muscarinic cholinergic

1. Promotion of dopamine synthesis receptors in the striatum

Levodopa Acetylcholine blocking drugs

Immediate metabolic precursor of dopamine

ADRs:
GIT-Anorexia, nausea and vomiting
Cardiovascular-cardiac arrhythmias

Behavioral effects
Dyskinesias and response fluctuations
Wearing-off reactions
On-off effect Seizure
Characterized by an excessive,
Carbidopa- dopa decarboxylase inhibitor
hypersynchronous discharge of cortical neuron
Prevent peripheral metabolism of levodopa
activity which can be measured by
electroencephalogram (EEG)
Pyridoxine –enhances the extracerebral
metabolism of levodopa
Three major phases:
Prodrome
Levodopa with MAO-A inhibitors- can cause
Ictal phase
hypertensive crises
Post ictal phase
2. Direct activation of dopamine receptors
Convulsion
Violent, involuntary contractions of the
Dopamine receptor agonists
voluntary muscles
Ergot derivatives
Bromocriptine and pergolide
Epilepsy
Non-ergolines
Pramipexole Chronic seizure disorder characterized by
Ropinirole seizures that usually recur unpredictably in the
Apomorphine absence of a consistent provoking factor

3. Prevention of dopamine degradation Seizure classification

I. Partial seizure
Monoamine oxidase inhibitors Most common seizure type
Selegiline Simple
Rasagiline Complex

Catechol-O-Methyltransferase inhibitors
Tolcapone II. Generalized seizure
Entacapone diffuse, affecting both cerebral hemispheres

4. Promotion of dopamine release Absence (petit mal)

-present as alterations of consciousness lasting
10-30 seconds
Amantadine
Antiviral agent
Myoclonic
-present as involuntary jerking movement

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SUMMATIVE LECTURE IN PHARMACOLOGY 1 Ms. Rizza A. Caluag

Felbamate
Tonic clonic (grand mal)
-most dramatic type of seizure Others
Levetiracetam
Clonic Retigabine
-characterized by sustained muscle contraction
alternating with relaxation

Tonic
-involve sustained tonic muscle extension

Atonic (drop attacks)

-sudden loss of postural tone

Antiepileptic drugs
Three main categories of therapeutics

Na channel blockers
Phenytoin
Fosphenytoin
Carbamazepine
Oxcarbazepine
Valproic acid
Lamotrigine
Topiramate
Zonisamide

Enhancement of GABA inhibition

Barbiturates
Phenobarbital
Primidone
Benzodiazepines
Diazepam
Lorazepam
Clonazepam
Clorazepate
Tiagabine
Stiripentol
Vigabatrin

Calcium channel blockers

Ethosuximide
Oxazolidinediones
Gabapentin
Pregabalin

Blockade of N-methyl-D-aspartate (NMDA)

glutamate receptors

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