1. Drug dosage forms and routes of administration
2. Information about drugs
3. Drug legislation in CZ
What is a dosage form?
It is a final form, in which
the drug is given to the patient.
Dosage Form
• Mixture of substances with therapeutical effect and
excipients
• Excipients: antioxidants, fillers, pigments (dyes), fragrances,
ointment bases, solvents etc.
• No pharmacological effect
• Allergies (parabens), intolerance (lactose)
• Shape and characteristics of a medical preparation
• Adjusted to the route of administration
• Influence pharmacokinetics of a medical substance
Generations of dosage forms:
1st = classic dosage forms
2nd = controlled release
3rd = controlled biodistribution
Excipients of AERIUS tablets:
Core: calcium hydrogen phosphate
dihydrate, microcrystalline cellulose,
maize starch, talc.
Coating: lactose monohydrate,
hypromellose, titanium dioxide,
macrogol 400, indigotin, carnauba
wax, white wax.
Classification of Dosage Forms
According to the
consistency:
• solid
• semi-solid
• liquid
• gaseous
According to the usage:
• for internal use (Ad usum
internum, e.g. Peroralia,
Parenteralia)
• for other use (Ad usum
alium, e.g. Ocularia,
Nasalia, Unguenta).
Liquid Dosage Forms
a) For internal use:
1. (Per)oral liquids
– solutions, suspension, emulsion for per os administration
– tinctures, drops, syrups
2. Parenteral liquids
– injections
– infusions
b) For external use:
– eye drops, ocular waters, ear drops, nasal drops
– liquids for cutaneous use, for compresses
– liquids applied to the mucosa (douche – irrigation, gargle)
Semi-solid Dosage Forms
 Applied on the skin or mucosa
 Local effect (dermatology)
 Systemic effect (TTS)
 Ointment (unguent)
 Creme
 Gel (jelly)
 Paste
 Transdermal patch
(TTS, Emplastra)
Solid Dosage Forms
Specific in shape:
 Tablet
 Suppository
 Vaginal pessary (suppository)
 Capsule
 Lozenge (pastilles)
Non-specific in shape:
 Dusting powder
 Herbal mixture
 Peroral powder:
• Classic
• Grained
• Effervescent
Tablets and Capsules
Tablets:
• Uncoated
• Coated
• Gastro-resistant
• Effervescent
• Tablets disperged in the
mouth
• Chewable
• Sublingual
• etc.
Capsules:
• Hard
• Soft
• Gastro-resistant
• With modified release
• etc.
Gaseous Dosage Forms =
Aerodispersions
Topical
• ear, nasal, oral, sublingual and cutaneous spray
Preparations for inhalation
• liquids (scattering of liquid drops)
• powders (particle size determines the place of
absorption)
Foams
• cutaneous, rectal, vaginal foams
Making of an aerodispersion:
• Mechanically by a nebulizer (spray)
• By liquefied/compressed gas (pressure container)
Routes of administration
Systemic administration
= drug is absorbed into the
circulation → it influences all
the body
• Enterální aplikace:
– enteral
– parenteral
Local (topical) administration
= drug is NOT absorbed into the
circulation → it affects only the
place of application
• :
– skin, mucosa, e.g. conjunctiva:
– GIT, but the drug in not
absorbed from GIT
How could a drug be administered?
Systemic administration – enteral
(Per)oral (per os, p.o.) Enteron (ancient greek) = intestine
• Onset of effect depends on phys-chem. properties of the
medical substance and excipients
• Possibility of lower bioavailability: first-pass effect (liver)
Rectal (per rectum)
• Do not irritate stomach, do not cause nausea
• Lower bioavailability – lesser surface of rectum walls
• Sooner onset of effect – plexus venosus rectalis flows into
vena cava inferior („bypass of the liver“)
„First pass“ effect
Systemic administration – parenteral
Para enteron (ancient greek) = out of the intestine
1. Non-injection (non-invasive)
a) oral
• Absorption by oral mucosa (e.g. subligual)
• Lipophilic substances – quick absorption (2 mins), e.g.
nitroglycerin
b) inhalation
• Gases, vapours nebo small particles
• Respiratory diseases (asthma, COPD...)
c) transdermal
• TTS = transdermal therapeutic system (controlled release)
• E.g. hormonal contraception patch, nicotine patch, analgesic patch
d) transnasal
• Good perfusion of nasal mucosa
• Substances could irritate it, or impair cilia function
• E.g. calcitonin, antimigraine drugs
e) vaginal – e.g. hormonal contraception ring
Systemic administration – parenteral
2. Injection (invasive)
- non-physiological
a) injection
• small volume of liquid
• i.v. administration – quick onset of effect
• i.m., s.c. – gradual absorption into circulation
b) infusion
• larger volume of liquid
• parenteral nutrition, minerals,
glucose, ATBs, cytostatics etc.
What is this tablet?
What is this drug used for?
How frequently should I use it?
What are possible adverse effects?
Who must not use it?
What is an appropriate dose?
How to store it?
Does it influence vigility?
Could this drug influence the effect of other drugs?
?
?
?
? ?
Information about Drugs
PIL & SPC
• PIL = patient information leaflet = package leaflet for patients
• SPC = summary of product characteristics = information for
medical specialists (physicians, pharmacists, nurses etc.)
EMA – European Medicine Agency (ema.europa.eu)
• Database of RMPs granted central authorisation by EC/EMA
• Reports concerning drugs‘ safety – alerts
• List of newly authorized drugs
SUKL – State Institute for Drug Control (sukl.eu)
• Database of RMP authorized in CZ
• Free access to all PILs and SPCs (in czech)
European Pharmacopoeia = european standard for the quality of
drugs (Czech Pharmacopoeia = text from EP + czech specialities)
Computer databases of medical preparations
• AISLP (czech↔english, in most pharmacies and doctor‘s offices)
Pharmacopoeia
• Purpose: to guarantee safe, effective and quality drugs
• Information about medical substances, excipients, dosage forms
• Instructions for production, preparation, control, storage of drugs
• Used mostly in pharma industry
What could we found there?
• Analytical and instrumental examination methods
• Materials for drug containers and cases
• Instructions to ensure sterility of medical preparations
• Instructions concerning radiopharmaceuticals, vaccines etc.
• Monographs of specific substances
• Tables with usual dosage of drugs in adults, children, animals
• etc.
NO: mechanism of actions, adverse effects, pharmacokinetics,
contraindications, pregnancy safety etc.!
Basic Drug Legislation in CZ
Act No. 378/2007 Coll., on pharmaceuticals
• Research
• Authorization of new drugs („registration“)
• Production, preparation and distribution
• Prescribing and dispense of medical preparations
• Destroying of unusable drugs
• Pharmacy duties
• Pharmacovigilance = drug safety service
• Controls and sanctions
Medical Prescription (Rx) in CZ
Validity:
• classic Rx: 14 days
• Rx for ATBs: 5 days
• Rx for local ATBs: 14 days
• Drugs of abuse and
psychotropic substances
(special Rx form): 14 days
• Rx for repeated use: 6 months,
max. 1 year
• Rx from ED: day after the day
of making up (= max. 48 h)
Legislation – Drugs of Abuse
Act No. 167/1998 Coll. on Dependency Producing
Substances & Order of the Government 463/2013 Coll.
regarding the lists of dependency producing substances
Specified narcotic and psychotropic drugs
should be strictly monitored:
• Keeping files of accepting and dispensing
– „Opiates Book“
• SUKL require this information
• Special Rx form – with oblique blue strip
• Medical preparations and Rx forms should
be stored in a safe or vault!
Classification of narcotics
Group 1 → Rx with blue strip
• Highly addictive
• E.g. strong opioid analgesics
• morphine
• oxycodone
• fentanyl etc.
Group 2
• Lower risk of addiction
• Classic Rx form
• E.g. codeine
Group 3 = „forbidden substances“
• No therapeutic use
• Misused
• Sometimes used in the research
• E.g. hashish, heroin etc..
Classification of psychotropic drugs
Group 1 = „forbidden substances“
• Hallucinogens, psychostimulants
• E.g. MDMA (exstasy)
Group 2 → Rx with blue strip
• Misused psychostimulants, addictive
• E.g. methamphetamine and other amphetamins
• Therapeutically used: e.g. methylphenidate, buprenorphine
Group 3
• Barbiturates, risk of addiction, limited therapeutic use
• E.g. pentobarbital
Group 4
• Benzodiazepines, barbiturates and other
potentially addictive drugs
• Classic Rx. form
• Hypnotics, sedatives, antiepileptics etc.
• E.g. diazepam, oxazepam, phenobarbital…
Precursors
= substances used in the production of addictive and
psychotropic substances
• classic Rx (except pseudoephedrine)
• ephedrine – nasal drops in sinusitis
• pseudoephedrine – medical preparation for cold treatment
→ OTC with restriction
• ergotamine – antimigraine suppositories
• ergometrine – obstetrics