Sources of Drug Standards and Information o Some drugs are destroyed by Gastrointestinal

1. USP – NF enzymes/juices
2. Remington’s Pharmaceutical Sciences - Prevented by: coating (enteric-coated tablet)
3. Merck Index - Administering drug after meals: food neutralize acid
4. Martindale – The Extra Pharmacopeia in the stomach therefore saving the drug
5. Handbook on Drug Interactions o Some drugs undergo first-pass effect: pass through liver
6. Handbook on Non-prescription drugs before site of action therefore decreasing its contents
7. Physician’s Desk Reference - Examples of drugs which undergo First-pass effect:
8. Journals – Pharmacy, Medicine, Nursing, etc. Morphine, Aspirin, Nitroglycerin
9. Drug inserts - Only oral drugs undergo FPE, so if possible, avoid oral
10. Internet route if FPE is undesired and choose other routes
o Some drugs are unpalatable which may lead to non-
PHARMACOKINETICS compliance
A. Definition/Description - Remedy: add flavoring
- Answers the question: What does the body do to the drug? - Place drug inside a capsule or coat it
- Deals with the movement of drugs in the body → time o Some drugs (Example: HCl and FeSO4) may stain or
coarse on the Administration, Distribution, Metabolism, and destroy the enamel of the teeth
Excretion o Patients may be uncooperative, unconscious, vomiting,
or have difficulty in swallowing (loss of gag reflex)
B. Route of Administration (ROA)
B.1. Factors affecting ROA 2. Topical route
2.1. Dermatological route
1. Intended site of action - How to enhance absorption on skin:
- Local: action of drug is on site of administration o Abrade or damage skin (CAUTION: Boric acid can
- Systemic: of drug is at the site of administration and also cause toxicity on damaged/denuded skin)
distal sites o Use of a fatty vehicle (wax, lanolin)
2. Rapidity & Duration of Action/Effect o Use a keratolytic agent (to soften skin and enhance
- 2 most rapid: Inhalation and Injection absorption of drug) – Salicyclic acid for treatment of
- Long effect: Implant corns/callus and warts
o Use of transdermal dosage form
3. Physical & Chemical Properties
→ Plaster (a medicated → Patch (medicated
- Example: Insulin – destroyed by proteases in GIT so it is or protective dressing that adhesive patch that is
given subcutaneously (parenteral) consists of a film (as of placed on the skin to deliver
- The action of some drugs depend on ROA cloth or plastic) spread a specific dose of medication
with a usually medicated through the skin and into the
→ Epsom Salt (MgSO4 ∙ 7H2O)
substance; something bloodstream; promotes
 Oral: laxative (stool softener) applied to heal and healing to an injured area of
 IV: anticonvulsant for patients with Eclampsia soothe) the body.)
(convulsion in pregnant women) 2.2. Mucosal route
 Topical: anti-inflammatory - No need enhance absorption for mucosal route
B.2. Routes of Administration because the route is already rich in capillaries (blood
1. Oral – preferred ROA: simple to use vessels) which will absorb drug
- Always need to be followed with liquid (preferable water) 3. Inhalation
- Convenient - Via the respiratory tract
- Economical: low cost - Patient: voluntary, on their own
- Limitations: - Form:
o Unpredictable absorption, distribution, metabolism, and → gas
excretion → liquid: in the form of a nebule; makes use of a
nebulizer, atomizer, or spray to reduce particle size
 → solid: in the form of a powder (micronized);
insufflations: makes use of insufflator
- Alveoli: increase surface area
- Systemic activity
- Deeper penetration to respiratory tract: ↓ PS
4. Parenteral
- Administered via injection which penetrates the skin
- 4 requirements for administration:
 Aspetic & Sterile Preparation which includes a
clean surface and the use of gloves, mask, etc.
 Critical regulation of dose
o IM (max): 5mL o SQ (max): 2mL
 Certain degree of technical skill
4.1. Intravenous
- Administered into the peripheral vein (Cephalic,
Basilic, Median cubital, and Radial veins), central vein
(Jugular vein or Subclavian vein) with the
requirement of technical skills
- Volume: 0.1mL to 1 Liter
- Types:
 Bolus IV: large single dosing
- slowly administered to allow the body to adjust
- dose: 10 – 50mL
 Intermittent IV – given at scheduled times
- Maximum dose: 150mL
 Intravenous fluid – maximum dose: 1 Liter which
is good for 48 hours
- Also known as Swero or Dextrose
- Uses of IV:
 To replace depleted blood volume with blood,
plasma expanders (such as Dextran)
 To supply nutrients and electrolytes for patients
who are not allowed to take in anything by mouth
 To prevent or relieve tissue dehydration: example
water for heat stroke patients
 To administer drugs such as Lidocaine (local
anesthetic, and treatment for dysrhythmia) and
Nitroprusside (in hypertensive emergency)
- Advantages of IV:
 Action & Effect of drug is immediate
 Dosage of drugs can be adjusted based on
patient’s response by adjusting number of drops
 Constant drug concentration (Steady state) can be
achieved by proper rate of administration
 Irritating drugs can be administered with minimal
trauma
 Can be used in patients who cannot swallow, are
unconscious, or in times of emergencies
- Disadvantages of IV:
 ADRs occur rapidly
 Once administered, drug cannot be retrieved
 Drugs given intravenously have many
incompatibilities with IVF
4.2. Intra-arterial
- Into the arteries
- Requirement: the one who would administer should
be an expert specially in anatomy to precisely locate
the artery
- Sites: Brachial and Inguinal
- Why IA: to have a higher concentration of drug in the
site of action: blood is already oxygenated so blood
directly goes to the site of action; unlike in
intravenous where the blood in which the drug was
administered in is deoxygenated so it first has to pass
the lungs so the amount of drug is decreased
- Dye: diagnostic agent
- Antineoplastic agent
4.3. Intramuscular
- Administered into the large muscle at a 90° angle
- Sites:
 Deltoid
 Vastus lateralis
 Gluteal or ventrogluteal
- Volume: at most 5mL
- Purpose of intramuscular administration: because
drugs are deposited into the muscle (depot) then they
are slowly released into the blood circulation to reach
site of action
- Techniques:
 Stretching – in obese patients
- By pressing down on administration site to
compress the subcutaneous layer above the
muscle
 Pinching – for malnourished or emaciated patients
and infants, and for patients who lack muscular
tissue
- Done by gathering the tissue before administering
the drug via injection
  Z-track method – for irritating and highly colored
injections
- By twisting the skin, tissues become displaced
and so if there is drug leakage, only a small part of
the tissue would be affected and not allow the
drug to fully leak out to the surface
- Disadvantages of IM injection:
 A blood vessel may be it and will cause a problem
(Thrombophlebitis: a blood clot caused by irritation
causes inflammation to the vein) by blocking a
blood vessel
 A nerve might be hit which can cause paresthesia
(tingling sensation)
- Absorption: blood vessels are responsible for
absorbing drug specially in highly perfused muscles
4.4. Subcutaneous
- Sites: in areas where the fatty layers is rich/high
o Abdomen
o Upper lateral arm
o Subscapular space
o Thighs
- Maximum volume: 2mL
- Purpose: administer drugs
- Enhance absorption for SC by:
 Massaging area of administration
 Warm the drug/injection
- Decrease absorption by:
 Applying a tourniquet which decreases blood
supple and oxygen content of the SC layer
 Administration of drugs SC with vasoconstrictor
 SC can also be a depot to lipid soluble drugs
- Modifications:
 Hypodermoclysis: aka Interstitial or Subcutaneous
infusion (large volume)
- Administering a large volume of solution through
subcutaneous tissue for rehydration
- Co-administer with hyaluronidase (an enzyme
which acts on hyaluronic acid which is like a
cement to cells in SC layer) to loosen SC layer
bounded by hyaluronic acid
- Example drugs: NSS and Glucose solutions
 Implants -SC tissues act as Depot for the slow
release of drugs
- May be in the form of a tablet or small pills
- Administered via injection or by making a small
incision on skin tissue of patient
- Duration: 3 – 6 months
- Example: Norplant® which in a contraceptive
4.5. Other parenteral routes
i. Intradermal
- Site: under the epidermis; into the dermis
- Volume: less than 1mL; usually 0.1mL
- Use: for skin sensitivity testing – This test requires
injecting a 26- to 30-guage (very thin) needle with
a tiny amount of allergen into the dermis layer of
your skin. If you are allergic to an allergen, you will
get a bump and redness where the allergen was
injected. After a short time, each skin test reaction
is measured for swelling and redness. A large
enough skin reaction is a positive skin test. This
means an allergy may exist to the allergen placed
at that site.
 Mantoux Tuberculin Skin Test - is the standard
method of determining whether a person is
infected with Mycobacterium tuberculosis.
- The TST is performed by injecting 0.1 ml of
tuberculin purified protein derivative (PPD) into
the inner surface of the forearm. The injection
should be made with a tuberculin syringe, with
the needle bevel facing upward. The TST is an
intradermal injection. When placed correctly,
the injection should produce a pale elevation of
the skin (a wheal) 6 to 10 mm in diameter.
- Specific site: forearm
ii. Intra-articular
- Site: joints
- Requires an expert in anatomy because drug
should reach the synovial fluid (to lubricate joints)
- Ex: Anti-inflammatory drugs; Sodium hyaluronate
(Euflexxa®)
Vasodilator drugs in the treatment of vasospasm
Thrombolytic drugs for treatment of embolism.
iii. Spinal
- How: patient lie in fetal position (knee-chin
position) to expose the spine where drug is to be
administered (specifically, where the syringe will
penetrate the arachnoid membrane and will cause
the CSF to leak out and cause headache)
 iii. a. Intrathecal - drug is to be administered into the viii. Intra-cerebral
arachnoid membrane and will cause the CSF to leak - Site: into the brain; bypasses the blood-brain
out and cause headache barrier
- 2nd top ROA for *Dyes in diagnostics
iii. b. Epidural – drug is deposited into the arachnoid
* Dye is injected to the carotid vein to see blood clot
space
ix. Intra-osseous
iv. Intra-peritoneal
- Site: into the bones
- Site: peritoneal area (abdominal cavity)
- Purpose: strengthen bone
- Only for animals
- Example: Atropine, Morphine, Heparin, Digoxin,
 Peritoneal dialysis – blood to be filtered is allowed to
Phenytoin, Naloxone, Diazepam, Lidocaine
pass through the peritoneum in cases of uremia
(urine in blood; clinical syndrome associated with
fluid, electrolyte, and hormone imbalances and
metabolic abnormalities, which develop in parallel
with deterioration of renal function) or azotemia
(abnormally high levels of nitrogen-containing
compounds in the blood) wherein the kidneys are not
functioning properly

v. Intrapleural
- Site: pleural cavity
- Example: antibiotic for treating infections in pleural
cavity - Penicillin may be injected in cases of lung
empyma (Pleural empyema is a collection of pus in
the pleural cavity caused by microorganisms,
usually bacteria)
 Near drowning – dirty water accumulate into the
pleural cavity caused by the lung extruding the fluids
and the negative pressure in the lungs do not allow
water to enter

vi. Intracardiac
- Site: directly into the heart (left ventricle)
- Epinephrine: jumpstart the heart after cardiac arrest
- Isoproterenol
- Adrenaline during cardiopulmonary resuscitation

vii. Intra-amniotic
- Site: amniotic fluid
- Purpose: terminate pregnancy → abortion
- Example of intra-amniotic abortifacient:
Prostaglandin F2-α and E2, Digoxin, Ethacridine
lactate (Rivanol®), Mifepristone + Misoprostol
 Amniocentesis - the sampling of amniotic fluid
using a hollow needle inserted into the uterus, to
screen for developmental abnormalities in a fetus.