L2 Principles in Pharmacology 2017

Principles of Pharmacology:
Drugs in Pharmaceutical Phase

Pharmacokinetics I - Overview
Types of Medications
HAZEL ANNE L. TABO

OUTLINE
Drugs in Pharmaceutical Phase
Principle of Pharmacology:
I. Pharmacokinetics
A,D,M,E
Types of Medication Orders
hal17.lovebio.lovelife
I. Pharmaceutical Phase oral dose
form
II. Pharmacokinetics what the body
does to the drug
III. Pharmacodynamics what the
drug does to the body
I. PHARMACEUTICAL PHASE
Drug administration or Dosage forms: oral,
ocular, nasal
Takes into account the intended mode of use
and also ensures ease of handling (e.g.,
stability, precision of dosing) by patients and
physicians.
Pharmaceutical technology is concerned with
the design of suitable product formulations
and quality control.
A. Liquid Prep
Solutions, suspensions (a sol or mixture of small water-
insoluble solid drug particles dispersed in water); Solutions
a) aqueous (water); b) alcoholic (types: drop regulated
in # drops, syrup measuring spoon; not precise dosing;
for direct absorption)
Emulsions (dispersion of minute droplets of a liquid agent
or a drug solution in another fluid, e.g., oil in water). Note:
Sedimentation results due storage (Suspensions &
Emulsions)
Eye drops and nose drops (mucosal surfaces of the eye
(conjunctival sac) & nasal cavity, respectively. Nasal drops
are more viscous to prolong contact time.
B. Solid dosage
Tablets, coated tablets & capsules
Tablets disk-like form (mg or less)
Effervescent tablet (compressed powders)
immediately dissolved in H2O and ingested as liquid
prep
Matrix-type drug-covered in matrix & released by
diffusion once moistened
Coated Tabs cored drug covered by a shell (waxy)
prevent degradation, mask bad taste/odor, easier
intake; color-coded
Capsules oblong-casing (gelatinous) with powdered
drug
Drug Administration: Release &
Absorption
Disintegration tablets break-up & capsules

open when moistened
Dissolution wet exposure for release (may
take time)
Liberation drug particle release can vary
(diffusive form)
Absorption pass through GI mucosa (by
intestines); solution forms in the stomach
Drug Form Drug Release
Matrix tab Lattice design slow leach by GI

fluids, release & absorption
proceeds as it reaches
intestinal route
Enteric-coated Coat thickness design whether
tablet release & absorption in
proximal / distal bowel (Ex:
dissolution in SI & release in
Colon)
Tablet / Capsule Film thickness (gradual
dissolution in enteral transit,
variable release & absorption)
Coated tab with Dividable ad libitum (fractions
delayed release of dose can be administered)
(slow-release Retarded release is for
tabs) undesirable rapid rise in blood
level or slow absorption is
needed for longer drug effect
Liquid form Direct stomach absorption
Parenteral bypasses
enteral absorption
Ampules (multiple / single use)
aspirated via syringe
Cartridge ampule special injector by needle
Infusion large dose for extended period
Aerosol gaseous solid/liquid particles
(micronized powder) in spray nozzle
Suppositories rectal /vag; oily film
spreads over mucosa & pass
Powder, ointment, pastes skin for
protection/care
Transdermal pasted to epidermis, drug
depot is non-invasive with admin same to
infusion
Injections (IV, IM, SC), have same
osmotic pressure & pH like body fluids
(avoid tissue damage at site)
From Oral to P-Kinetics
Absorption Drug in Distribution Drug in
Drug release
Systemic Tissue
DISSOLUTION
Circulation Organ
Elimination
Pharmacologic
Metabolism
or
Excretion
Clinical effect
II. Pharmacokinetics
What happens to the drug after it has been
taken; Dose-concentration
Indicates the movement of drug molecules
across cell membrane (CM) during ADME.
Drug transfer is dependent on the composition
and structure of cell membrane
How much of the administered dose reaches the
blood stream and the target sites of action
How much of the drug gets sequestered or
destroyed in the body
Figure 3-1. The relationship between dose and effect can be
separated into pharmacokinetic and pharmacodynamic components
(Katzung and Trevor 2015).
Pharmacokinetics
Pharmacokinetics
The process by which
drugs moves in order to
achieve drug action.
Involves (4) processes:
1. Absorption (input)
2. Distribution
3. Metabolism
4. Elimination
Four (4) Processes of Pharmacokinetics
1. Absorption the movement of drug particles

from the GIT to body fluids by passive diffusion,
active transport and pinocytosis
- Involves major transmembrane processes
- Important site Stomach; lumen of GI
2. Distribution the process by which drugs

distribute itself and becomes available to the
body fluids & tissues. It is influenced by blood
flow & its affinity to the tissue & protein binding
effect (bioavailability).
Plasma half-life the time it takes for the
amount of drug to be reduced to one-half (50%)
of drug concentration in plasma concentration.
Pharmacokinetics: I. Absorption
1.1. Passive absorption occurs mostly by diffusion
without energy requirement from high concentration
to low concentration (solute>H2O H2O>solute)
1.2. Active absorption a carrier-mediated process

through the use of enzymes or protein to move
against concentrated agents (low to high
concentration). Carriers follow principle of enzyme
kinetics.
1.3. Pinocytosis engulfs the drug to carry it across

the membrane (cell-drinking condition).
Passive transport : DIFFUSION MOVEMENT
PLASMALEMMA
Low concentration
High concentration
If 1 side of membrane is unequal: Left side no. of forward moving vehicle or [high] is
greater than backward moving vehicle or [low], thus movement is from high to low
concentration (2nd law of thermodynamics)
If 2 sides of the membrane have equal concentration: allows steady state
concentration of drug = no net transfer of drug across CM (forward molecules are
balanced by backward molecules)
CARRIER-MEDIATED TRANSPORT
GI Lumen Intestinal Epithelium Blood
CARRIER
Drug Drug
Drug
CARRIER
Drug-Carrier complex - shuttles the drug across CM and
dissociate drug into the other side of the membrane.
Roles of membrane transporters (T) in pharmacokinetics.
T play roles in pharmacokinetic pathways (drug absorption, distribution,
metabolism, and excretion), thereby setting systemic drug levels. Drug
levels often drive therapeutic and adverse drug effects.
Carrier-mediated: Facilitated Diffusion &
Active transport
Moves along concentration gradient using a

vehicle (carrier)
Features of Carrier system (Active transport
and facilitated diffusion):
Saturability
Drug selectivity
Kinetic competition of drugs with similar
structures (analogs)
Beckers World of Cell, 2012
GLOMERULUS
BOWMANS CAPSULE
Kidney section, Masons stain, 1000x
3. Metabolism or Biotransformation Liver (as the 1o site of metabolism)
whereby most drugs are inactivated by hepatic enzymes converted or
transformed inactive metabolite or a water-soluble substance for excretion.
- converts drug into useful form or detoxified into water-soluble form via renal
elimination.
- First pass effect a phenomenon wherein due to passage of drug in liver,
some enzymes convert the drug into metabolites before they can reach the
target tissues to give its effect. Drugs should be designed to withstand hepatic
first-pass effect.
4. Excretion or Elimination Kidney (main route of drug elimination) together
with minor routes such as the bile, feces, saliva, sweat and breast milk.
1. A stat order indicates that medication has to
be given immediately and only once.
2. The single order - a medication to be given
once a specified time.
3. A standing order may or may not have
termination date.
4. A p.r.n. (pro re nata) - an order permits the
nurse to give a medication when in his/her
judgment the patient requires it.
1. A stat order: to be given immediately and
only at once. (Metoclopramide 10mg/tab.
1 tab. now).
2. The single order: to be given once a

specified time. (Metoclopramide 10mg/tab.
1 tab. 1hr prior to OR).
3. A standing order: may or may not have
termination date. (Metoclopramide
10mg/tab. 1 tab. TID a.c. as
coordinated).
4. A p.r.n. permits the nurse to give a
medication when his/her judgment in the
patient requires it.
(Metoclopramide 10mg/tab. 1 tab. each
vomiting not to exceed 6 tabs/day).

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Uploaded by

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Principles of Pharmacology:

Drugs in Pharmaceutical Phase

HAZEL ANNE L. TABO

Disintegration tablets break-up & capsules

Matrix tab Lattice design slow leach by GI

1. Absorption the movement of drug particles

2. Distribution the process by which drugs

1.2. Active absorption a carrier-mediated process

1.3. Pinocytosis engulfs the drug to carry it across

GI Lumen Intestinal Epithelium Blood

Moves along concentration gradient using a

2. The single order: to be given once a

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