Pharma Trans 1,2,6

- Into to basic pharmacology - "Rational Drug Therapy / Ethical Consideration in Drug Prescribing - Nature and Sources of Drugs and Dosage forms

WHO definition of Rational Drug Therapy

• Medication appropriate to clinical needs

• Doses meet their own individual requirements (for a period of time)

• Lowest cost

Considerations in Ethical Prescribing

• Evaluate and define the patients problem + Give a diagnosis

• Determine the therapeutic objectives of drug therapy

Prescribing decisions should be based on the primary

diagnosis and relevant secondary diagnosis.

• primary diagnosis

• relevant secondary diagnosis.

pharmacokinetic vs pharmacodynamic

• Pharmacokinetics (PK): What the body does to the drug.

• Pharmacodynamics (PD): What the drug does to the body.

Process of rational drug prescribing

1. identifying the problem/diagnosis

2. establishing the therapeutic goals

3. choosing the drug using the ESSC criteria,

4. writing the correct prescription, counseling and monitoring the patient.

Involved in compounding, preparation, collection, standardization and dispensing of the drugs

Pharmacy

• Study of crude drugs, proper horticulture, harvesting and uses of materials derived from nature

• physical and chemical properties of the drugs with the description and identification of their sources and nature

Pharmacognosy

Study of how the chemical structure of the drug is related to physiological, biological, and biochemical effects

Biochemorphology

Study of the harmful effects of drugs and other chemicals on human, animals, and plants

Toxicology

Deals with dosage of the drug required to produce a therapeutic response

Posology

Studies the mechanism of action of a drug at the enzymatic level

Molecular Pharmacology

T or F? Substitutions within the chemical structure of the drug may lead to either low toxicity or lethal toxicity

True

Factors affecting biochemorphology:

○ Protein-Binding

○ Drug Solubility

○ Acidity / Alkalinity

• Also known as Clinical Therapeutics

● Deals with rational development of drugs, their safe and effective use, and other proper evaluation of drugs in humans for prevention, diagnosis, treatment, alleviation or cure of a disease.

● Refers to rational drug prescribing

Clinical Pharmacology

What is the average amount of time it takes for an experimental drug to travel from the lab to the medicine chest?

12 years

Out of 5,000 preclinical compounds evaluated

• how many typically make it to human clinical trials?

• How many get approved?

5 enter human trials; only 1 gets approved.

What are the sample sizes for the three primary phases of clinical trials?

• Phase I: 20 to 80 healthy volunteers.

• Phase II: 100 to 300 patient volunteers.

• Phase III: 1,000 to 3,000 patient volunteers.

What application must be submitted to the FDA before human testing can begin, and what is filed after Phase III is successful?

IND (Investigational New Drug application) before human testing

NDA (New Drug Application) after Phase III.

Which phase of clinical trials experiences the highest rate of drug failure?

Phase II (only 25% of innovative drugs move on to Phase II).

What is the primary purpose of Phase IV trials, and who reports the findings?

Post-marketing surveillance to detect rare/long-term toxicities, patterns of drug utilization, or new indications. It is done by all physicians.

What does EUA stand for, and what is its purpose?

Emergency Use Authorization; it allows for the use of unregistered drugs or vaccines during public emergencies (without skipping strict safety standards).

Define the term "Placebo."

A substance or treatment with no active therapeutic effect used as a methodological tool in medical research.

True or False: A placebo response can only lead to psychological changes, not objective physiological or biochemical changes.

False. The placebo response may involve objective, physiologic, and biochemical changes in addition to changes in subjective complaints.

What action do Cathartic drugs do?

increase bowel movement (stronger than laxatives)

• entire evacuation of entire colon

Phase 4 of clinical trials establishes the drug's:

a. Over-all safety

b. Additional unusual side effects

c. Short term side effects and risks

d. Efficacy in patients with the disease

Short term side effects and risks

Generally, the duration for an experimental compound to be studied and

be out in the market for public use takes:

a. 1 year

b. 3 years

c. 6 years

d. 12 years

d. 12 years

12. Which is part of the pharmacokinetics phase of a drug?

a. Biotransformation

b. Tablet disintegration

c. Mechanism of action

d. Drug-drug interactions

Biotransformation

The strength of a drug required to produce effect is:

a. Efficacy

b. Potency

c. Effectiveness

d. Bioavailability

Potency

For a prescription with several ingredients, this is used as the solvent of a

solution to increase the bulk of a mixture:

a. Basis

b. Vehicle

c. Adjuvant

d. Corrective

b. Vehicle

Drugs that need prescription by licensed physicians

• Opioids

• Hallucinogens

• Stimulants

• Depressants

• Anabolic steroids

Outline of P-drug selection

1. Diagnosis

2. Therapeutic objectives

3. Non-drug measure

4. inventory of effective drug groups

📌The ___ total score (drug group 2) would be your P-drug group.

highest

T or F? Excipients has NO physiologic or pharmacologic effect on patient.

T

What do you call inactive substances that help bulk-up formulations that contain active ingredients.

Excipients

T or F? Drugs > 1000 Mw in size can diffuse readily

False!

• drugs must @ least be 1000 MW

• Any more than 1000 do NOT DIFFUSE

T or F? Most useful drugs are CHIRAL (enantiomers) molecules

T

what is the fundamental requirement for a drug's shape to produce a pharmacological effect?

Complementary to receptor site

Based on the structural diagrams in Figure 3 of the notes, how many distinct diastereomers exist for the drug Ephedrine?

4

How does the potency of dextromethamphetamine compare to its levo counterpart in inhibiting noradrenaline reuptake?

10x more

What proportion of clinically useful drugs are described as chiral molecules in the provided material?

More than half (NOT ALL)

Which specific pharmacological mechanism is inhibited by dextromethamphetamine?

Noradrenaline reuptake

the difference between Ephedrine and Pseudoephedrine is based on their status as:

Diasteromers

• have multiple chiral centers

• NOT mirror images of each other

what is a regulated substance in the Philippines but OTC in the United States?

D. Ephendrine

Atropine, vinblastine, vincristine, quinine,

colchicine, and morphine are all examples of?

Alkaloids

Where is Lanolin obtained from?

Sebaceous gland of wool bearing animals

Where is Cyanocobalamin obtained from?

Animal liver

Streptomycin is derived from which microorganism?

Streptomyces gryceus

Chloramphenicol is derived from which microorganism?

Streptomyces venezuelae

T or F? Microorganisms play an integral role in genetically engineered drugs

True

_ is used as Laxatives

• Magnesium sulfate

• magnesium trisilicate

• Magnesium sulfate

_ is used as antacids

• Magnesium sulfate

• magnesium trisilicate

• magnesium trisilicate

_ drugs are more inexpesnive and can be mass produced.

Synthetic drugs

Aspirin is a synthetic derivative of ?

Salicyclic acid

Can be used to diagnose bone, heart or other organ

problems

• Technitium Tc99

• Iridium-192

• Technitium Tc99

Can be inserted inside or near a tumor to kill cancer

cells while sparing neighboring cells.

• Technitium Tc99

• Iridium-192

• Iridium-192

Para sa Bobo:

• PKinetics is the journey the medicine takes to move in, around, and out of your body!

• PDynamics is the magic action the medicine does to make your fever go away or stop your tummy from hurting!

___form is considered by default as the gold standard for having a 100% bioavailability,

Intravenous

What is Bioavailability?

Fraction (percentage) of an administered drug that successfully reaches the systemic circulation (bloodstream) in its unchanged, active form.

3 major classes of Routes

• Enteral (via GI tract)

• Parenteral ( injections)

• Topical / Localized

Route	Onset	Bioavailability	Key Characteristic / Trade-off
IV	Fastest	100% (Gold Standard)	Directly enters bloodstream; no absorption step needed.
Oral (PO)	Slow	Variable (5 to <100)	Most convenient; subject to significant first-pass liver metabolism.
IM / SC	Moderate	High (75 to <100%))	IM allows larger volumes than SC; both can cause pain.
Inhalation	Very Rapid	Variable	Hits lung blood supply almost instantly.
Transdermal	Very Slow	High (80 to < 100%)	Avoids first-pass effect; long-lasting, steady drug delivery.

For oral medication, which organ reduces bioavailability?

Liver

Which route is the slowest BUT avoids the first-pass effect and lasts a long time?

Transdermal

T or F? Sterile solutions can initially be in powder form

because they are unstable when reconstituted.

T

What is the preferred route for gaseous and volatile

drugs (anesthetics)?

Pulmonary