Pharmacology ▪ Median Lethal Dose (LD )

2yr - 1st sem, midterms ▫ is the dose of drug that will be lethal in
50% of a group of animals.
PHARMACODYNAMICS
PHARMACODYNAMICS
➢ “Pharmaco” - medicine
➢ "Dynamics" - change
“What the drug does to the body?”
● Dose Response Curves
● Effect on site (Receptors)
● Chemical response
❑ THERAPEUTIC INDEX
▪ estimates the margin of safety of a drug through
DOSE- RESPONSE CURVES
the use of a ratio that measures the ED50 and
❖ TERMINOLOGIES
the LD50.
Idiosyncratic reaction
▪ FORMULA :
- unique, unusual, and unexpected response to a
drug
TI =
Paradoxical Reaction
- opposite effect from what is intended.
Anaphylactic reaction
- severe, possibly fatal, allergic reaction.
Placebo Effect
- the more the patient feels positive about certain
medications being taken, the more positive the
physical response.
❑ FREQUENCY DISTRIBUTION CURVE
▪ Median Effective Dose (ED ) 50
▫ is the dose required to produce a
specific therapeutic response in 50% of
a group of clients

⌑ NARROW TI
○ Sample NTI Meds
◦ warfarin
◦ levothyroxine
◦ carbamazepin
e
◦ Digoxin
◦ lithium
carbonate
◦ phenytoin
◦ Theophylline

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 ⌑ WIDE TI C. morphine (30mg)
○ Sample WTI Meds ↳ Only drug C relieves headache
◦ Most antibiotics effectively.
◦ β-lactams ❑ DOSE-EFFECT PARAMETERS
◦ Macrolides
◦ Quinolones

❑ DOSE-EFFECT PARAMETERS
▪ POTENCY
▫ the dose of medication required to
produce a particular response
▪ EFFICACY or INTRINSIC ACTIVITY
▫ The maximum effect
▫ *more important than potency

RECEPTORS & DRUG ACTION

❖ TERMINOLOGIES
○ Sample scenario SPECIFICITY (SELECTIVITY)
◦ Two common over-the-counter (OTC) - How specific the drug is for a particular type of
analgesics receptor
A. ibuprofen (Advil, Motrin; 200 - ↑ SPECIFICITY = ↓ Side Effects
mg) and AFFINITY
B. acetylsalicylic acid (Aspirin; - attraction between drug and a receptor
650 mg). - ↑ Affinity = ↑ binding capacity even at lower
↳ Both relieves headache and are equally concentration
effective - ↓ Affinity = needs higher concentration to
❑ DOSE-RESPONSE CURSE bind.
RECEPTORS
- are specific proteins, situated either in cell
membranes or, in some cases, in the cellular
cytoplasm.
- is the specific chemical constituent of the cell
with which a drug interacts to produce it’s
pharmacological effects.
○ Sample scenario ❖ THEORIES OF DRUG ACTION
◦ You are caring for a patient with 1. Fischer’s ‘Lock and Key’ Hypothesis
end-stage cancer complaining of severe - Drugs that will fit into the receptor
headache. have an “affinity” for that receptor-site
A. ibuprofen (Advil, Motrin; 200 → PRODUCE EFFECT
mg) and 2. Koshland’s ‘Induced-Fit’ Hypothesis
B. acetylsalicylic acid (Aspirin;
650 mg)

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 - binding of a substrate to an enzyme
causes a change in the shape of the
Drug causing Antidote Memory trick
enzyme so as to enhance or inhibit its toxicity
activity. (hand in glove model)
OPIOIDS Naloxone NO more Opioids
(Narcan→Opioids)
DRUG-RECEPTORS INTERACTIONS
❖ DRUG-RECEPTORS INTERACTIONS WARFARIN Vitamin K During WAR, vit K
1. Agonist Kills WARfarin
- A drug that produces the same type of
HEPARIN Protamine You will need HELP
response as the endogenous substance
sulfate from a PRO to stop
- they possess both affinity and efficacy bleeding out
○ Sample :
◦ Bethanechol BETA Glucagon Beta blockers be GONe
◦ Acethylcholine BLOCKERS with glucaGON
2. Antagonist BENZODIAZE Flumazenil I FLU fast in my
- a drug will occupy a receptor and -PINE mercedes BENZ
prevent the endogenous chemical from
ACETAMINO Acetylcysteine ACETaminophen→AC
acting
PHEN ETylcysteine
- do NOT change the → receptor they
have affinity but NO efficacy MAGNESIUM Calcium MAGgie CALLs for
SULFATE Gluconate help!
DRUG- DRUG INTERACTIONS (MAGnesium→CALciu
m)
❑ SYNERGISM
⬝ combination of two or more drugs which IRON Deferoxamine DeFERexamine→FERr
produced effect greater than the effect of TOXICITY ous means “containing
individual drugs. iron”
⬝ (1+1=3)
○ Sample RECEPTORS REGULATIONS
1. DESENSITIZATION
- cells stop responding to the increased
dose of hormone/neurotransmitter
- leads to tolerance
2. HYPER-SENSITIZATION
- cells make new receptors and shift them
to the surface of the cell.
❑ POTENTIATION - REBOUND EFFECT
⬝ 2 drugs wherein Drug A multiplies the “idle”
effect of Drug B
TAKE AWAY
⬝ (1+0=2)
➢ Pharmacodynamics is how drugs produce
❑ ANTAGONISM
change in clients and the differences in client
⬝ 2 drugs OPPOSING each other wherein Drug
responses to medications.
A cancels out the effect of Drug B
➢ The therapeutic index, expressed
⬝ Usually employed when drug toxicity occurs
mathematically as is a value representing the
⬝ (1+1=0)
margin of safety of a drug. The higher the
⬝ ex) naloxone is given for opioid toxicity
therapeutic index, the safer the drug.

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 ➢ The graded dose-response relationship describes
how the therapeutic response to a drug changes
as the medication dose is increased.
➢ Potency, the dose of medication required to
produce a particular response, and efficacy, the
magnitude of maximum response to a drug, are
means of comparing medications.
➢ Drug receptor theory is used to explain the
mechanism of action of many medications.
➢ Agonists, partial agonists, and antagonists are
substances that compete with drugs for receptor
binding and can cause drug-drug and food-drug
interactions.

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