PHARMACOLOGY by Kate

2nd Year, 1st Sem: Prelims AY 2023-2024

○ Done to test if may asthma talaga ang patient

OVERVIEW OF HISTORY
● Babylonians, Greeks, Egyptians, Chinese
○ Used plants to relieve symptoms of disease
■ Morphine
● Galing sa Papaver somniferum (analgesic)
■ Digoxin (for heart failure)
○ Papyrus Ebers
■ Egyptian medical papyrus of herbal knowledge
■ Opium (Opium Poppy) - Analgesic
○ PH - Halamang Gamot (BABY PLANTS)
● Pharmacology was recognized as a distinct discipline when the first department of
pharmacology was established in Estonia (North America) in 1897.
● John Jacob Abel
○ Father of American Pharmacology
○ Founded the first Pharmacology in the US in the University of Michigan in 1890.
CONCEPTS
PHARMACY
● Greek words: Pharmakon (drugs or medicine) and logos (study)
● Study of chemicals/drugs in living tissues (humans/animals) and how these chemicals
help diagnose, treat, cure, and prevent disease (prophylaxis) or correct the
pathophysiology of living tissues.
● Effects, Faith/Disposition, Clinical Uses of drugs
DRUG
● Any article that is used in the diagnosis, mitigation, treatment, cure of diseases
● Functional Modifier
○ Alter the biochemical and physiological processes/activities of the cell
○ Common function of drugs
● Replenisher
○ Supplement insufficient endogenic compounds
○ Ex. Hypothyroidism - kulang sa iodine kaya nagbibigay ang doctor ng iodine
○ Diabetes Mellitus Type 1 (Insulin Dependent) - kulang ang insulin production sa
katawan kaya binibigyan ng insulin (subcutaneous)
● Diagnostic Agent (Ex. Dobutamine and Methacholine)
○ Dobutamine (pharmacologic stress test, heart - treadmill pero if walang paa
given ito to papagod the patient)
○ Methacholine - Cholinergic agent (DUMBELS)
○ Side effects is difficulty of breathing
● Chemotherapeutic Agent
○ Kill or inhibit the growth of foreign cells in the body
○ -cidal - kill
○ -static - inhibit
○ Chemotherapeutic Agent is yung maraming "anti" (Antibiotic, Antifungal,
Antiviral)
○ Bactericidal - Bacteria ang pinapatay
○ Bacteriostatic - Inhibit growth
● Usually listed in: USP (United States Pharmacopeia) or BP
○ Basis sa ingredients na ginagamit sa making ng gamot
● Action of Drug
○ Chemical changes or effects that a drug has on the body cells or tissues
○ Mechanism of Action (MOA)
● Indication
○ Documented usefulness if a specific drug to combat or treat certain diseases
● Contraindication
○ List of conditions for which a drug should not be given
● Side Effects
○ Additional effects of the drug that is not necessarily the main purpose of giving
the drug
○ Not always bad ito like sa minoxidil for hypertension, increases hair growth. So
it is has a topical preparation para sa alopecia
○ Usual negative but there are some beneficial effects
○ Off label use of the drug
○ Metformin - papayat ka raw here but it may cause lactic acidosis if nasobrahan
(rare case but not zero chance of happening)
● Receptor
○ Molecule that is the target of pharmacologically-active substances
PHYSICAL NATURE OF DRUGS
● Drug molecule must have the appropriate size, electrical charge, shape, and atomic
composition.
● A drug is often administered at a location distant from its intended side of action
(except pag topical kasi doon na mismo ang site of action)
○ Systemic absorption
● Physical state of the drug often determined the best route of administration (ROA)
● Drug Size - For specificity of action and mobility of drug in the body
○ Alteplase: Thrombolytic (Thrombo - blood clot; lytic - destroy) (intra-atrial) - For
px MI/stroke
○ Not always good kasi if there is a clot it compromises blood flow which can
cause MI/stroke
● Drug Reactivity and Receptor Bonds ○ Too costly or super rare disease
○ Determine the duration of effect ● Illicit drugs
○ Covalent - ASA (Aspirin) Acetylsalicylic Acid ○ Drugs that are regulated or prohibited
■ COX 1 and COX 2 - irreversible ○ MDMA - ecstasy
■ APAP - paracetamol ○ Cocaine
○ Electrostatic Bonding - H bonds and VDW (vander ekmerut)
○ Hydrophobic Bonding - for highly lipophilic (Lipo - lipid, Philic - loving) drugs LEGAL REGULATION OF DRUGS
● Drug Shape
○ Permits binding to the receptor FDA PREGNANCY CATEGORIES
○ "Lock-and-key" theory CATEGORY A ● Adequate and well-controlled studies have failed to demonstrate a risk
■ Kung saan siya mas magfi-fit or complement to the fetus in the first trimester of pregnancy (and there is no evidence
■ Induced-fit Theory of risk in later trimesters). (SAFE)
○ Chirality/Stereoisomer (Carvedilol; Thalidomide) ● Ex.: levothyroxine, folic acid, liothyronine
■ Isomers (R or S) yang dalawa, S sa Carvedilol then S sa Thalidomide eh CATEGORY B ● Animal reproduction studies have failed to demonstrate a risk to the
nag-cause ng disaster (S 4 SATAN) fetus and there are no adequate and well-controlled studies in
pregnant women.
SOURCES OF DRUGS ● Ex.: metformin hydrochlorothiazide, cyclobenzaprine, amoxicillin
● May studies pero no effect on animals
● Minerals
CATEGORY C ● Animal reproduction studies have shown an adverse effect on the
○ Kremil s or any antacid (aluminum or magnesium)
fetus and there are no adequate and well-controlled studies in
○ If aluminum only magkaka- constipation
humans, but potential benefits may warrant use of the drug in pregnant
○ If magnesium only magtatae
women despite potential risks.
● Salts or inorganic compounds
● Ex.: gabapentin, amlodipine, trazodone
○ Gold is used for rheumatoid arthritis (oral or parenteral)
● May effect sa animals
● Animals
○ Insulin is from pig CATEGORY D ● There is positive evidence of human fetal risk based on adverse
● Plants reaction data from investigational or marketing experience or studies in
○ Synthetic sources humans, but potential benefits may warrant use of the drug in pregnant
○ Aspirin is from the bark of willow tree women despite potential risks.
● Ex.: losartan
● Benefits outweighs the risk
CLASSIFICATION OF DRUGS CATEGORY X ● Studies in animals or humans have demonstrated fetal abnormalities
● Prescription drugs (rx - recipe, takethou) versus OTC drugs (over the counter, and/or there is poor evidence of human fetal risk based on adverse
no need for prescription like APAP (biogesic)) reaction data from investigational or may experience, and the risks
○ AMR - antimicrobial resistance like sa antibiotics involved in use of the drug in pregnant women clearly outweigh
○ dapat di lagi mag OTC drugs like herbal supplements like MX3 kasi marami potential benefits.
siyang claims pero not approved therapeutic claims and baka mamask yung ● Ex.: atorvastatin, simvastatin, methotrexate, finasteride
symptoms
○ Paracetamol - "ingat" sa overdose “What differentiates a drug from poison?” The amount of dose.
● Investigational drugs
○ Drug development:
■ Pre clinical - animals
■ Clinical - tao, subjects for trial use (4 phases) dito yung investigational
drugs

● Orphan drugs CONTROLLED SUBSTANCES

○ Drugs na for rare diseases

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 ● Robitussin has codeine noon which is from (morphine) opium poppy
● I - Most potential for abuse and dependence; no medicinal qualities
● II - High; Some medicinal qualities
● III - Moderate; Doctor’s prescription required
● IV - Low; RX required; Fewer refill regulations
● V - Lowest; Acceptable; RX required; Fewest refill regulations

DRUG NAMES
● Generic name (official name) vs. Trade name (brand name)
○ Official name
○ Trade name - nagbabago like biogesic sa manufacturer may branded at
generic eh mas appealing pag branded like sa color, texture but they have the
same effect
○ Generic - Paracetamol; Trade Name - Biogesic, Bioflu
● Chemical name
○ ASA - Acetylsalicylic acid
○ APAP - acetyl para aminophenol

BRANCHES/FIELDS OF STUDY
PHARMACEUTICS
● Science of the medicine's design: formulation, manufacturing, stability, and
effectiveness.
● Some compounds have placebo like OCP

PHARMACOTHERAPEUTICS
● Concerned with the clinical uses of drugs
● RPHx to RN - NCP to study the drugs
● Decrease cost and drug interactions

PHARMACOGNOSY
● Science that deals with the study of drugs derived from natural sources
(plants/animals)
● 10 HALAMANG GAMOT (BABY PLANTS)

PHARMACOVIGILANCE
● Science and activities relating to the detection, assessment, understanding, and
prevention of adverse effects or any other medication, vaccine related problem
● Refers to continuous monitoring of unwanted effects and other safety- related aspects
of marketed drugs
● ex. Thalidomide in 1900's - si preggy has a problem kaya pumunta sa asawa and sabi
may morning sickness and nag-alala si hubby kaya nagpunta sa drug store. nabigyan
● RA 9165 - No Marijuana ng Thalidomide then returned to preggy who took the medicine. effective for morning

Pharmacology by Kate Piedad 3

 sickness but 9 months later, nanganak siya pero no limbs which is called phocomelia
amelia. si S-isomer ang naibigay hindi sa R- isomer.

PHARMACOEPIDEMIOLOGY
● Study of both the beneficial and adverse effects of drug on large number of people
● Policies

TOXICOLOGY
● Study of toxic effects
● Branch of pharmacology which deals with the undesirable effects of chemicals on
living systems
● Antidotes: APAP - if greater than 4g pwedeng magka risk of hepatotoxicity
● Ang antidote ay N-AC (n acetylcysteine) which is a mucolytic

PHARMACOKINETICS
● pharma - drugs, kinetics - movement
● What the body does to the drug fate and disposition of drugs in the body PHARMACOKINETICS
● FATE: absorbed, distributed, metabolized, eliminated/excreted
● Study of the fate/disposition of a drug
● First pass effect is agad namemetabolize kaya merong drugs na parenteral which
● What the body does to drugs
goes to the systemic circulation agad
● Absorption, Distribution, Metabolism, Excretion (ME is under ELIMINATION)
● ADME/LADMERT
○ ADME - absorbed, distributed, metabolized, eliminated/excreted
○ LADMERT - liberation, absorpiton, distrimution, response, toxicity ABSORPTION
● Transfer of drug from its site of administration to the bloodstream
PHARMACODYNAMICS ● Physical factors in influencing absorption
● D FOR DRUGS ○ Blood flow to the absorption site
● What the drug does to the body: how the drugs produce its effect on the body ○ Total surface area available for absorption
● Molecular MOA (mechanism of action), drug-receptor interaction, dose-response ■ Sa small intestine usually kasi it contains villi/ microvilli which stretches
curve and increases total surface area for absorption
● Metabolism - liver; Excretion - kidneys ○ Contact time at the absorption surface

ACTIVE VS. PASSIVE TRANSPORT

DIFFERENCES ACTIVE TRANSPORT PASSIVE TRANSPORT
Energy Requirement ✔ ATP Simple Diffusion:X
Facilitated Diffusion: X
Carrier Mediated ✔ Simple Diffusion:X
Facilitated Diffusion: ✔
Saturable ✔ Simple Diffusion:X
Facilitated Diffusion: ✔
● Active needs ATP because it goes against the concentration gradient and passive
goes along with it
● Carrier mediated (usually protein) - yes to active tapos sa faci diffusion need ng carrier
sa simple hindi
● Saturable - yes to atp (mapupuno) but simple no pero sa faci yes

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 DRUG DISTRIBUTION DURING PREGNANCY AND LACTATION
BIOAVAILABILITY (F)
● Drug distribution during pregnancy and lactation is also unique.
● Fraction of administered drug in a chemically unchanged form that reaches the ○ It is important to know who the patient is because some drugs may go in the
systemic circulation placenta which may lead to toxicity.
○ Chemically unchanged is yung di pa na-metabolize ○ Morphine
○ Parenteral = 100% ■ Papaver somniferum/opium poppy
○ Oral < 100% (FPE - first pass effect ng liver) ■ Analgesic (pain reliever)
○ Other routes ≤100% ■ If baby receives morphine, the baby will have withdrawal effects after birth
● How much of a 500mg dose of bioavailable if the administered drug has an F of 75% ■ Side effects: diarrhea
● FACTORS THAT INFLUENCES BIOAVAILABILITY ■ Loperamide - constipated para di magtae
○ First-pass hepatic metabolism ■ If diarrhea, mag-ORS to replenish. Diarrhea compensates for excretion of
○ Solubility of the drug toxins in the body.
○ Chemical instability (LUNA HIPE) ● During pregnancy, most drugs cross the placenta and may affect the fetus.
○ Nature of drug formulation ● During lactation, many drugs enter the breast milk and may affect the nursing infant.

LUNA HIPE WHICH IS PREFERRED?

Lipophilic Hydrophilic
Unionized Ionized Molecular Size High MW Low MW
Non Polar Polar Lipid Solubility Highly lipid soluble Lowly lipid soluble
Absorbed Excreted Drug half-life Longer 150 Shorter 150
Protein Free Bound
DISTRIBUTION pKa Low pKa High pka
● It is the process by which a drug reversibly leaves the bloodstream and enters the
● High Molecular weight dapat para di makapasok sa placenta
interstitium (extracellular fluid) and/or the cells of the tissues.
● Low lipid soluble - agad nailalabas
● Once a drug is injected or absorbed into the bloodstream, it is carried by the blood and
● pKa - measurement of acidity
tissue fluids to its sites of pharmacologic action, metabolism, and excretion.
● FACTORS AFFECTING DISTRIBUTION
○ Blood flow (cells at work) METABOLISM
○ Capillary structure ● Metabolism is the method by which drugs are inactived or biotransformed by the body
■ Integrity of blood vessels affect blood flow (HIPE).
○ Binding of drugs to CHON (proteins; volumes of distribution) ● Most often, an active drug is changed into one or more inactive metabolites, which are
■ Albumin - type of protein where acidic drugs bind (ASA binds to Albumin) then excreted
■ Drug Interactions (drug-drag) ● Detoxification
● Bound - inactive; binding of drugs; may cause toxicity ○ Involves conversion of foreign agents (xenobiotics) into substances of less
● Free/Unbound - active; distribution potential toxicity (HIPE)
■ Nurses are the last line of drug interaction (administer) ● Metabolism
○ Relative hydrophobicity of the drug ○ Sum of chemical changes in living cells by which energy is provided for vital
■ May drugs na ayaw sa tubig processes and activities and new materials are produced and assimilated for
■ LUNA HIPE growth and maintenance (biochem definition)
● Important in knowing why drugs are not that effective and why ● Biotransformation
some drugs take effect agad ○ Process by which chemical reactions carried out by the body convert a drug
● LUN - Absorbed (distributed) into a compound different from that administered originally
● HIP - Excreted (metabolized) ○ May drugs na active maba-biotransformed into toxic
● Why should a drug undergo biotransformation?

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 ○ To convert a drug into a more excretable form
○ To convert a pharmacologically active drug to inactive metabolite
○ To convert an active drug to an active metabolite
○ To convert an inactive drug to an active metabolite
○ To convert a drug into a more toxic metabolite
● APAP - paracetamol
● Phases of Metabolism
● Phase I and II
● GOOD SIDE
○ Babies are able to metabolize paracetamol through sulfation
○ Glucuronidation - soon lang sa adults
○ Sulfation and glucuronidation causes detoxification and elimination
● BAD SIDE
○ 12g - 15g ang overdose sa paracetamol (toxic, lethal)
○ Enzymes are saturated (nababawasan) mag undergo ng oxidation
○ Delikadong ma-oxidize ang paracetamol sa body which causes NAPQI (toxic
metabolite of APAP)
○ Glutathione helps at some point however, hepatotoxicity (liver) happens when
glutathione saturates
○ Antidote: N-acetylcysteine which replenishes glutathione
Pharmacology by Kate Piedad
PRODRUGS
● Drugs that are inactive are converted to active forms
● Reasons:
○ To improve unfavorable physical properties
■ Chloramphenicol - drug of choice for typhoid fever
■ Super pait kaya ginawa nilang prodrug which turned into its salt form (for
appealing taste)
○ To improve unfavorable pharmacokinetics properties
■ ACE inhibitors (CEL - Captopril, Enalaprilat, Lisinopril) for hypertension
○ Prodrug approach is more efficient and cheaper
KINETICS OF DRUG BIOTRANSFORMATION
FIRST-ORDER KINETICS
● Metabolic transformation of drugs is catalyzed by enzymes.
● The rate of drug metabolism is directly proportional to the concentration of free drug
● Example: Most drugs
ZERO-ORDER KINETICS
● The rate of drug metabolism remains constant over time
● A constant drug amount is metabolized per unit time
● Example: TAAPES - Theophylline, Alcohol, Aspirin, Phenytoin, Ethanol, Suspension
○ Theophylline - family of coffee. madederive dito ang tes. for asthma/respiratory
○ Alcohol and Ethanol - drug solvent
○ Phenytoin - anticonvulsant
○ Suspension - drug formulation
● First-Order - directly proportional (pumapasok = lumalabas)
● Zero-Order - rate of elimination is constant
REACTIONS OF DRUG BIOTRANSFORMATION
6
PHASE I ○ Enzyme: Sulfotransferase
● Function to convert lipophilic molecules into more polar molecules (HIPE) by ● Methylation
introducing or unmasking a polar functional group ○ Enzyme: Methyltransferases
● Functionalization ○ Nonpolar, inductive
○ Introduction of a new functional group ■ COMT MAOi
● Phase I reactions are functionalization reactions, frequently adding a new oxygen ■ Catecholamine
atom or exposing an existing functional group ■ MA Oxidase inhibitors
■ Catecholamines - Epinephrine, Norepinephrine, Dopamine. DA sa CNS.
OXIDATION Epi at NE sa sympa (fight or flight)
● Addition of oxygen or removal of hydrogen (H2) from the original compound
● Carried out by a group of monooxygenase (oxidative enzymes found in the hepatic ENZYME INDUCTION ENZYME INHIBITION
ER), mainly CYP450 enzymes ● Involves protein synthesis,needs time ● Decrease of the rate of metabolism of a
up to 3 weeks to reach a maximal effect drug by another one; leading to toxicity
REDUCTION ↑ enzyme = ↑ metabolism ↓ enzyme = ↓ metabolism
● The removal of oxygen or the adding of hydrogen to the original compound (↓ plasma concentration) (↑ plasma concentration)
● Enzymes responsible are usually located in the cytoplasm Result: ↓ activity Result: ↑ activity
PHASE II (CONJUGATION) Example: St. John’s wort Example: Grapefruit juice
● Glucuronidation
○ Most common and most important inducible, reduced activity in neonates (1-
28/30 days) BIOTRANSFORMATION
■ Chloramphenicol - typhoid fever ● Most drugs are biotransformed before being eliminated
■ It will undergo glucuronidation which is wala sa bata. Naibigay sa babies ● Drug metabolites are generally more polar than their present compound
(sulfation) kaya nagkaroon ng gray baby syndrome. ● Concurrent ingestion of two or more drugs can affect the rate of metabolism of one or
○ Enzyme: Glucuronyltransferase more of them
● Acetylation
○ Enzyme: N-Acetyltransferase ELIMINATION
■ Isoniazid - kasama sa RIPE/HRZE (TB)
● Rifampicin, Isoniazid, Pyrazinamide, Ethambutol
● Undergoes acetylation
○ Slow Acetylators - African, American, Egyptians, Caucasians
○ Fast Acetylators - Asian, Eskimos
■ 2 px with TB: African (low dose kasi slow metabolization) and Filipino
(high dose kasi fast metabolization)
● Glycine Conjugation
○ Transformation of Benzoic Acid to Hippuric Acid
● Glutathione Conjugation
○ Enzyme: Glutathione-S-Transferase
■ Endogenous, potent, and powerful oxidant
● Drugs have finite duration of action (DOA) in the body
■ 100% gluta can’t be administered orally. If meron man, synthetic lang
● Elimination process (biotransformation and excretion) are major determinants of this
‘yon.
duration
■ Gluta is administered through IV! (antioxidant siya)
● Renal and fecal excretion are the most important routes for drug elimination
■ Side effect: whitening of skin
● Free drug (not bound to albumin) flows through the capillary slits into the Bowman's
■ Main effect: serves as antioxidant
space as part of the glomerular filtrate. Lipid solubility and pH do not influence the
● Sulfation
passage of drugs into the glomerular filtrate.
○ Present at birth
● Creatinine Clearance

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 ○ Used to assess any renal impairment and indicate whether drug doses need be ■ Beta 2 - lungs
reduced if renal excretion is an important component of drug elimination. ● Antagonist
■ Dapat mailabas yung creatinine kasi it's a waste substance (kidney's ○ A drug that binds w/o activating its receptor and thereby blocking and
state of function) preventing
○ A normal result is to 0.7 to 1.3 mg/dL (61.9 to 114.9 µmol/L) for men and 0.6 to ○ Propanolol (BB - Beta Blocker)
1.1 mg/dL. (53 to 97.2 µmol/L) for women ● Partial Agonist
○ A drug that binds its receptor but produces a smaller effect event at full dosage
CLEARANCE ○ Ex: Nalbuphine (narcotic)
● Volume of plasma that is cleared per unit time ○ If combined with full agonist it will become an antagonist
● Low clearance = Toxicity
● High clearance = Decrease Activity TYPES OF DRUG INTERACTION
● Some drug conjugates are hydrolyzed in the lower gastrointestinal tract back to the ADDITION
parent compound and reabsorbed in the process referred to as enterohepatic
circulation, which extends the duration of drug action. ● The response yielded by combined drugs is equal to the combined responses of
individual drugs (1 + 1 = 2)
● Example: Alcohol + CNS Depressants (both sedative)
PHARMACODYNAMICS SYNERGISM
● The response elicited by combined drugs is greater than the combined responses of
● What the drug does to the body individual drugs (1 + 1 = 3)
● Example: Sulfamethoxazole + Trimethoprim (Cotrimoxazole)
A. Drug-Receptor Interactions
B. Drug-Response Relationships POTENTIATION
C. Molecular Mechanism of Actions ● A drug which has no effect on the system enhances the effect of the other (1 + 0 = 2)
● Example: Amoxicillin + Clavulanic Acid (No antibacterial effect)
DRUG-RECEPTOR INTERACTIONS
● Receptor ANTAGONISM
○ A molecule to which a drug binds to bring about a change of the biologic ● Drug inhibits the effect of another due to opposite pharmacological actions
system ● Example: Warfarin + Vitamin K
● Receptor Site
○ Specific region of the receptor molecule to which the drug binds MECHANISMS OF ANTAGONISM
● Affinity ● FUNCTIONAL ANTAGONISM
○ Ability to bind; describes how strongly the drug and receptor interact ○ Occurs when two ligands (drugs) bind to different receptors and produces
● Intrinsic Activity effects
○ Ability to activate the receptor ○ Example: Norepinephrine & Acetylcholine
● Efficacy ■ Norepinephrine is a beta 1 receptor (stimulation of beta 1 receptor)
■

○ Maximal effect an agonist can produce SYMPATHETIC PARASYMPATHETIC

● Potency Ach Ach
○ Quantifies the amount of drug to produce a given effect Ne Ach
■ 50 percent of efficacy is potency ■ Acetylcholine has muscarinic receptors (m1, m2, m3) - parehas na may
■ Maximum effect is efficacy effect sa heart pero different effect
● Agonist ■ Epinephrine for anaphylactic shock (where in may low BP) but doesn't
○ A drug that activates its receptor upon binding affect the histamine receptor
■ Beta 1 - increases the activity of the heart ● RECEPTOR ANTAGONISM
■ inject norepinephrine then it will bind with B1 and activate it (ex. septic ○ Occurs when two ligands (drugs) bind to same receptors and produces
shock) opposite effects

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 ○ Example: Norepinephrine + Propranolol ● Location: Cell Membrane
○ Norepi is B1 agonist ● Discus: Gs, Gi, Gq
○ Propranolol is non-selective ○ Q - Qontraction
■ Antagonist/blocker of B1 and B2 ○ I - Inhibitory
○ Inderal - For Mitral Valve Prolapse ○ S - cAMP
■ Caused shortness of breath SYMPATHETIC PARASYMPATHETIC
● CHEMICAL ANTAGONISM Receptors L1 L2 B1 B2 M1 M2 M3
○ Neutralization, chelation G GQ GI GS GS GQ GI GQ
○ Example: Protamine Sulfate
○ Antidote for heparin (blood thinner/anticoagulant) Type 3: Enzyme-linked Receptors
○ Watch out for bleeding kasi ayaw nito for platelet which clots kaya need ng
● aka: Kinase-linked Receptors Location: Cell Membrane
protamine
● Examples: Insulin receptors, Growth factor receptors
○ Insulin is produced by beta cells of pancreas (islets of Langerhans)
DRUG-RESPONSE RELATIONSHIPS ○ Alpha cells produce glucagon
GRADED-DOSE RESPONSE
● A graph increasing response to increasing drug concentration or dose
○ Dapat therapeutic ang effect pero di maiwasan ang toxic since nothing's
absolutely safe Type 4: Gene-transcription Receptors
○ The graph: habang mas maraming drug concentration, mas maraming efficacy ● aka: Nuclear Receptors (Nuclear receptors kasi sa nucleus sila magi-interact)
○ Ex. 5 mg causes analgesic and 50% of the effect is the potency ● Location: Nucleus
● MOA: Gene Expression
QUANTAL-DOSE RESPONSE CURVE ● Examples: Steroidal Hormone, Thyroid Hormones
● A graph of the increasing fraction of a population that shows a specified response at
progressively increasing doses
○ 50 percent effective, 50 percent toxic dose CALCULATION OF DOSAGE AND SOLUTIONS
○ Narrow therapeutic drugs/ index
TOPIC OUTLINE
A. Systems of Measurement D. Calculation of Injectable Dosages
MOLECULAR MECHANISM OF ACTIONS B. Methods of Calculation E. Calculation of Intravenous Dosages
Type 1: Ligand-gated ion Receptors C. Calculation of Oral Dosage Forms F. Common Abbreviations in Drug
● Also called as lonotropic Administration
● MOA: Ion Influx
○ Changes the concentration gradient pagpasok or pagkabind ng meds sa SYSTEMS OF MEASUREMENT
protein
● Location: Cell Membrane
● Examples: GABA-A Receptor, Nicotinic Receptor METRIC SYSTEM (FORMER)
○ (lorazepam, diazepam, pwede for seizures), Nicotinic Receptor (skeletal ● Clear and simple
muscle relaxant) ● International Systems of Units
● international recognized decimal system of weights and measures
Type 2: G-protein coupled Receptors
● aka: Metabotropic, 7-transmembrane, Serpentine Receptors MEASURE OF LENGTH
● MOA: Needs secondary messengers to elicit response ● Meter is the primary unit of length in the SI
○ Phospholipid bilayer before the receptor. If an agonist/ligand binds to it, in the ● Table of the metric length
long run it will produce a secondary messenger ○ 1 kilometer (km) = 1,000 meters
○ Example: beta blocker ○ 1 hectometer (hm) = 100 meters

Pharmacology by Kate Piedad 9

 ○ 1 dekameter (dam) = 10 meters Example 3: 1 dam to m
T G M Km h da m dm cm mm mc nn
1 decimeter (dm) = 0,100 meter
1 centimeter (cm) = 0.010 meter 0
1 millimeter (mm) = 0.001 meter 10 m
1 micrometer (um) = 0.000,001 meter 1 dam= −1 -1 - 0 = 1 zero (positive) 1 x 10 = 10 m
1 nanometer (nm) = 0.000,000,001 meter
10 dam

The table may also be written: MEASURE OF VOLUME

1 meter = 0.001 kilometer ● The liter is the primary unit of volume. It represents the volume of the cube of one
= 0.01 hectometer tenth of a meter, that is, of 1 dm³.
= 0.1 dekameter
= 10 decimeters The table of metric volume:
= 100 centimeters 1 kiloliter (kl.) = 1000.000 liters
= 1000 millimeters 1 hectoliter (hL.) = 100.000 liters
= 1,000,000 micrometers 1 dekaliter (dal) = 10.000 liters
= 1,000,000,000 nanometers 1 liter (L) = 1.000 liter
1 deciliter (dL) = 0.100 liter
1 centiliter (cl.) = 0.010 liter
Equivalencies of the most common length denominations: 1 milliliter (ml.) = 0.001 liter
1000 millimeters (mm) = 100 centimeters (cm) 1 microliter (L) = 0.000,001 liter
100 centimeters (cm) = 1 meter (m)
TL GL ML KL hL dal L dL cL mL mcL nnL
T G M Km h da dm cm mm mc nn 1015 109 106 103 102 101 0 10-1 10-2 10-3 10-6 10-9
1015 109 106 103 102 101 0 10-1 10-2 10-3 10-6 10-9
Example 1: 10 dl to mL
Note: 10 0 0 = 1000 mL
Positive (+) - multiply −3
Negative (-) - divide 1 0 mL
10 dL= −1 -1 - -3 = 2 (100) 10 x 100 = 1000 mL
1 0 dL
Example 1: 1 km to m
T G M Km h da m dm cm mm mc nn Example 2: 5 mL to L
. 0 0 5 mL
1000 m 0
10 L 5
1 km= =1000 m 5 mL= -3 - 0 = -3 (1000) =0.005 L
1 km −3
1 0 mL 1000
Example 2: 1 hm to m
MEASURE OF WEIGHT
T G M Km h da m dm cm mm mc nn
Tg Gg Mg Kg hg dag g dg cg mg mcg nng
0 1015 109 106 103 102 101 0 10-1 10-2 10-3 10-6 10-9
10 m
1 hm= 2 2 - 0 = 2 zeroes (positive) 1 x 100 = 100 m
1 0 hm Example 1: 1 kg to g
1 0 0 0 = 1000 g

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 0
10 g
1 kg= 3 3 - 0 = 3 (1000) 1 x 1000 = 1000 g
1 0 kg

APOTHECARY SYSTEM
● US
● Commonly used in the past by pharmacists and physicians for compounding.
● Example: Morphine SO4, Atropine SO4, Codeine, Na Phenobarbital, ASA
● Largely replaced but still commonly used in household

APOTHECARIES’ FLUID MEASURE 2. How many drops would be prescribed in each dose of a liquid medicine if 20 mL
60 minims (m) = 1 fluidrachm or fluidram (f3 or 3)° contained 60 doses? The dispensing dropper calibrates 35 gtts per mL.12 gtts
8 fluidrachms (480 minims) = 1 fluidounce 3. Tetracycline has been shown to form a Calcium complex in bone- forming tissue in
16 fluidounces = 1 pint (pt) infants given oral Tetracycline in doses of 0.011 g/lb body weight every 6 hours.
2 pints (32 fluidounces) = 1 quart (qt) Express the dose in terms of mg/kg of body weight. 24.2 mg/kg
4 quarts (8 pints) = 1 gallon (1 gal) 4. Nitrostat Sublingual tablets are available as 1/200 gr tablets. What is the
approximate equivalent in milligrams? 0.325 mg
APOTHECARIES’ MEASURE OF WEIGHT
20 grains (gr) = 1 scruple (8) CALCULATION BASED ON PATIENT PARAMETERS
3 scruples (60 grains) = 1 drachm or dram (3) BASED ON AGE
8 drachms (480 grains) = 1 ounce (3) YOUNG’S RULE, BASED ON AGE
12 ounces (3760 grams) = 1 pound (ltr) Age
x Adult Dose=Dose for Child
Age+ 12
HOUSEHOLD SYSTEM
1 mL = 20 gtts (when calibrated; when drop rate is not given) COWLING’S RULE
1 tsp = 5 mL
Age at next birthday (¿ years) x Adult Dose
1 dessert spoon = 8 mL =Dose for Child
1 tbsp = 15 mL 24
1 wine glass = 60 mL
1 teacup = 120 mL FRIED’S RULE FOR INFANTS
1 tumbler = 240 mL Age (¿ months) x Adult Dose
1 glassful = 250 ml =Dose for Infant
150
SAMPLE PROBLEMS: CLARK'S RULE, BASED ON WEIGHT
1. A capsule contains the following amounts of medicinal substances: 0.075 g, 20 Weight (¿ lb) x Adult Dose
mg, 0.0005 g, 4 mg, and 500 g. What is the total weight of the substances in the =Dose for Child
capsule? 500.0995 g 150(average weight of adult ∈lb)
Note: The value of 150 in Fried's rule was an estimate of the age (12.5 years or 150
months) of an individual who would normally receive an adult dose, and the number 150 in
Clark's rule was an estimate of the weight of an individual who likewise would receive an
adult dose.

SAMPLE PROBLEMS:

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 1. The usual initial dose of chlorambucil is 150 mcg/kg of body weight. How many 2. If 3 tablets contain 975 milligrams of aspirin, how many milligrams should be
mg should be administered to a person weighing 154 lb? 10.5 mg contained in 12 tablets? 3900 mg
3. Sudafed cough syrup contains 0.09 of Dextrometorphan HBr in each fluidounce.
How many milligrams of this agent would bermaya present in each teaspoonful
dose? 15.22 mg

CALCULATION OF INJECTABLE DOSAGES

1. The adult intravenous (IV) dose of Zidovudine is 2mg/kg q4h daily. How many mg
will a 180-lb patient receive daily? 981.84 mg
2. If an insulin injection contains 100 units of insulin in each milliliter, how many
milliliters should be injected to receive 40 units of insulin? 0.4 mL

CALCULATION OF IV DOSAGES
1. The infusion rate of Theophylline established for neonate is 0.08 mg/kg/hr. How
many mg of drug are needed for a 12-hr infusion bottle if the body weight is 16 lb?
7 mg
2. An ICU medical order reads, "KCI 40 mEq in 1 liter N/S. Infuse at 0.5 mEq/min."
How many minutes will this bottle last on the patient? 80 minutes

BASED ON BSA (FORMULA AND NOMOGRAM)

2
Patient ' s BSA (m )
Patient Dose= 2
x Drug Dose (mg)
1.73 m
SAMPLE PROBLEMS:
1. If the adult dose of a drug is 100 mg. Calculate the approximate dose for a child
with BSA of 0.83 m^2.

COMMON ABBREVIATIONS

CALCULATION OF ORAL DOSAGES

SAMPLE PROBLEMS:
1. If the adult dose of a medication is 2 teaspoonsful (tsp.), calculate the dose for a
child if it is 1/4 of the adult dose. ½ tsp

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