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Pharmacology 1+2 > Lab 3 > Flashcards

Lab 3 Flashcards

1
Q

Ointment - Definition

A

Ointments are semi-solid dosage forms able to treat skin and mucosa. They contain the components homogenously dispersed (solved, suspended, emulgeated) in an ointment base.
– Homogenous
– Do not dissolve at body temperature
– Do not contain solid particles

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2
Q

Differents bw. ointments and cream, pasta and gel

A

-Cream: contains more water, than ointment
-Paste: contains a large proportion of solid powder finely
dispersed (also oral application)
-Gel: Gels consist of liquids gelled by means of suitable gelling agents (also oral application).

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3
Q

Ointment - Usage

A

– Local administration

– Systemic effect: high lipophilicity or appropriate vehicle (e.g. DMSO)

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4
Q

Ointment - Composition

A 
- Active compounds: antibiotic, antimicotic, antiviral
agent, NSAID’s, glucocorticoids, antihistamin, coating,
disinfecting agents etc.
-Ointment base components: Ingredients without or with low water solubility:
* Plant and animal lipids
* Hydrocarbons
* Waxes & wax alcohols
- Water soluble ingredients:
*Plants and animal polymers
*Synthetic polymers
- Hydrophobic ointments
- Water-emulsifying ointments
- Hydrophilic ointments
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5
Q

Ointment - Examples on plant and animal lipids

A
  • Fats
  • Cocoa butter (Fatty bases Theobroma Oil BP)
  • Oils (sunflower oils, castor oil, flax oil, cod-liver oil etc.)
  • Hydrolysis: glycerol, fatty acids
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6
Q

Ointment - Examples on hydrocarbons

A
  • Soft paraffin
  • Liquid paraffin
  • Hard paraffin
  • Vaseline
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7
Q

Ointment - Examples on waxes & wax alcohols

A 
• Wool wax (adeps lanae)
(hydrous wool fat, Lanolin 25% water)
 Lanalcol, Wool-fat alcohol
• Honey bee wax
 Myristyl alcohol
• Sperm Whale wax
(Physeter macrocephalus)
 Cetostearyl alcohol
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8
Q

Ointment - Examples on plants and animal polymers

A
  • Methylcellulose
  • Hydroxiaethylcellulose
  • Agar
  • Gelatine
  • Starch: potato, wheat etc.
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9
Q

Ointment - Examples on synthetic polymers

A
  • Macrogols (polyoxyethylenes)

* Polysorbates (Tweens)

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10
Q

Ointment - hydrophobic ointments; types and advantages/disadvantages

A

– White soft paraffin and yellow soft paraffin can be used as ointment bases.
– In case of skin irritation or when protective effects is needed.
– The disadvantage of paraffin usage on the skin is the prevention of the skin from perspiration

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11
Q

Water-emulsifying ointments

A 
– Water emulsifying hydrocarbon waxes and ointments, capable of oil-in-water emulsion formation:
• anionic emulsifying wax
• nonionic emulsifying wax
• cetomacrogol emulsifying ointment 
• anionic emulsifying ointment
– Water-emulsifying hydrocarbons, capable of water-in-oil
emulsion formation:
• simple ointment,
• paraffin ointment
• hydrous ointment.
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12
Q

Hydrophilic ointments

A

– Are miscible with water
– They can be applied when greater body surface area is
treated or when the ill animal is sensitive to hydrocarbons.

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13
Q

What are macrogol ointment?

A

Hydrophilic oitmentcontains that contains two types of polyethylene glycols; macrogol 4000 and macrogol 300.

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14
Q

Ointment - Dispensation

A
  • Jar

* Tube

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15
Q

Ointment - Prescription

A

„For external use only!”
• Official preparations (BP)
• Prepared preparations
• Licensed preparations

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16
Q

Eye ointment - Definition

A

Sterile, soft, homogenous ointments intended for application to the conjunctiva. Prolonged effect (eye-drops), a bit more preferable in cats (nasolacrimal duct).

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17
Q

Eye ointment - Composition

A
  • Active substance: AB, glucocorticoids, Vit. A, etc.

* Eye ointment bases: simple eye ointment, hydrous eye ointment

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18
Q

Eye ointment - Dispensation

A

– Not more than 5-10 grams (open package stability)

– In sterilised tubes with a cannula

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19
Q

Eye ointment - Prescription

A

– Official preparations
– Prepared preparations
– Licensed preparations

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20
Q

Oral gel and oral paste - Usage

A

– Orally

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21
Q

Oral gel and oral paste - Composition

A
  • Active substance: anthelminthics, AB, sedatives, probiotics etc.
  • Vehicle: gel or paste
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22
Q

Intramammary preparations - Definition

A

Sterile, soft preparations (suspensions, emulsions, solution) able to treat or prevent the diseases of the mammary gland.
They can be introduced into the mammary gland via the teat canal.
– Dry-cows = non-lactating cows
– Lactating cows

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23
Q

Intramammary preparations - Usage

A

– Udderwash
– Udder-disinfection
– Milking-out

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24
Q

Intramammary preparations - importances in case of lactating/dry animals

A

– In case of lactating animals, after 12 hours milk-out, then reapplication
– Dry cows: after last milk-out, long WP!

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25
Q

Intramammary preparations - Composition

A

– Active compound: AB, antimycotics, antiseptics, GC (their form changes whether lactating or not!)
– Vehicle: liquid paraffin, beeswax etc.
– Auxiliary subst.: stabilizing suspension and emulsion (eg. DMSO), preservatives (eg. Benzyl alcohol)

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26
Q

Intramammary preparations - Dispensation

A

– Plastic syringes with special injector (single doses)
– For the treatment of a SINGLE teat canal
– /Rarely multidose formulations/

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27
Q

Intramammary preparations - Prescription

A

– Official preparations (BPV) - rare!

– Licensed preparations

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28
Q

Suppositories - Definition

A

Solid, single-dose preparations, that will dissolve on body temperature.
The shape, volume and consistency are suitable for rectal administration (+ vaginal formulations)

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29
Q

Suppositories - Usage

A

– Mainly in small animals
– Local effect: disinfectant, adstringent, emolliating
– Systemic effect: sedative, anticonvulsive, NSAID’s etc.
(avoiding liver first pass)

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30
Q

Suppositories - Composition

A
  • Active substance: e.g. sedative, NSAID (powder or liquid)

* Suppository bases: hard fat , cocoa butter, supplemented hard fat, macrogol mass

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31
Q

Suppositories - Dispensation

A

Aluminium foils + box

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32
Q

Suppositories - Prescription

A

– Official preparations
– Prepared preprations
– Licensed preparations

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33
Q

Electuaries - Usage:

A

– Orally

– Not precise: only safe ingredients

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34
Q

Electuaries - Composition

A
  • Active substance: powder form, safe

* Vehicle: syrup (prepared), jam (homemade)

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35
Q

What are tranquilizers?

A

sedatives / neuroleptics (phenothiazines, butirophenons,Rauwolfia alkaloids)

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36
Q

Tranquilizer sedatives - Pharmacological effects

A
  • decreased motoric activity, decreased aggression
  • reduced response to stimuli and fear, indifference to the surroundings
  • No analgesic activity, but they potentiate the activity of analgesics (neuroleptanalgesia) ↔ slight analgesic activity can be observed by butyrophenones
  • Increasing the dose lengthens the duration of sedation, not the depth (they do not cause hypnosis)
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37
Q

Tranquilizer sedatives - Receptorial effects

A
  • Anti – α1-activity: hypotension (!) – horse: paradox-reaction
  • Anti – dopamine activity: mainly responsible for sedative effect. Antiemetic effect. PRL-secretion increases: contraindicated for pseudopregnant animals
  • Anti – histamine (H1) activity: antiallergic effect
  • Anti – serotonine activity: versatile actions, e.g. inhibited regulation of body temp.
  • Anti-muscarine effect: constipation, dry mouth (markedly in humans)
  • FSH-secretion decreases: fertility rate decreases
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38
Q

Tranquilizer sedatives - Side effects

A
  • Hypotension: can cause collapse in severely dehydrated, exsiccated animals (boxers very sensitive!)
  • Paradox-reaction might be present in the horse
  • Tissue irritation (e.g. chlorpromazine can cause muscle necrosis given im.)
  • They can induce epileptic seizures (anti-D-effect)
  • Hypothermia in cold places, hyperthermia in hot places
  • Can exacerbate the symptoms of pseudopregnancy
  • Slow metabolism and excretion: must not be given directly before slaughtering
  • Can cause penis-prolapse in stallions (especially propionilpromazine, acepromazine)
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39
Q

Tranquilizer sedatives - Indications

A
  • Sedation (e.g. transportation, capturing)
  • Antiemetic (against vomiting and nausea)
  • Neuroleptanalgesia in combination
40
Q

Tranquilizer sedatives - Active substances

A 
a) Phenothiazines: used to treat schizophrenia and manifestations of psychotic disorders:
– Chlorpromazine
– Propionil-promazine
– Acepromazine
– Thiethylperazine
– Promethazine
b) Butyrophenones: induce a state of apathy and mental detachment in patients with dysharmonious brain function
• Azaperone
• Droperidol
• Fluanison
41
Q

Tranquilizer sedatives - Chlorpromazine:

A

-Type of phenothiazine
-Chlorpromazini hydrochloridum
-Paradox-r., muscle necrosis, very slow excretion from the body
• A.U.V.: -
• Human:

42
Q

Tranquilizer sedatives - Propionil-promazine

A

-Type of phenothiazine
• A.U.V.: -
• Human: -

43
Q

Tranquilizer sedatives - Acepromazine

A

-Type of phenothiazine
-The time to reach maximal effect depends on the formulation (gels↔tablets)
• A.U.V.: ACP inj., tablet, Vetranquil inj., Sedalin oral gel
• Human: -

44
Q

Tranquilizer sedatives - Thiethylperazine

A

-Type of phenothiazine
-Pronounced antiemetic activity
• A.U.V.: -
• Human: Torecan inj., dragee, suppository

45
Q

Tranquilizer sedatives - Promethazine

A

-Type of phenothiazine
-Promethazini hydrochloridum
-Pronounced antihistamine activity
• A.U.V.: -
• Human: Phenergan (Pipolphen) tablets, inj., suppositories

46
Q

Tranquilizer sedatives - Butyrophenones

A
  • Slight analgesic activity!
  • Compensation of the respiratory depressant effect of opiates excellent for neuroleptanalgesia (e.g. droperidol + fentanyl) –> Cardiovascular depression and inhibition of temperature centre is less.
47
Q

Tranquilizer sedatives - Azaperone

A

-Type of butyrophenone
-For sedation of pigs, reducing the stress (i.m!)
• A.U.V.: Stresnil inj.
• Human: -

48
Q

Tranquilizer sedatives - Droperidol

A

-Type of butyrophenone
-Droperidolum
-Neuroleptanalgesia
• A.U.V.: -
• Human: Inapsine inj.

49
Q

Tranquilizer sedatives - Fluanison

A

-Type of butyrophenone
-Neuroleptanalgesia, especially in small, laboratory animals
• A.U.V.: Hypnorm inj. (+fentanyl)
• Human: -

50
Q

LIQUID DOSAGE FORMS - definition

A

Disperse systems where different liquids are used as dispersive phase.

51
Q

LIQUID DOSAGE FORMS - types

A
  • Homogeneous disperse systems: Solution
  • Intermediate categories: Emulsoid (Microemulsion), Suspensoid (Microsuspension)
  • Non-homogeneous disperse systems: Emulsion, Suspension
52
Q

Solution - DEFINITION

A
  • Homogeneous liquid system, clear (transparent) and free from particles and deposit
  • Ingredients are dissolved in suitable liquid vehicle
53
Q

Solution - USAGE

A
  • Oral: local or systemic effect
  • Uterine or udder treatment
  • Topical treatment of skin and mucous membranes
  • Ophtalmic use
  • Ear drop, nasal drop
  • Injection, infusion
54
Q

Solution - “Sterile solutions” and “isotonic and isohydric”

A

for parenteral use or for the treatment of mucous membrane of eye, vagina,
uterus and udder
- Injections, infusions, intramammary products and
eye drops have to be isotonic and isohydric

55
Q

Solution - CONTAINERS

A
  • Vials, Glass, Bottle, Plastic flask
  • Plastic tops or special closers, children resistant
    closer (mainly for elixirs, syrups), multidose formulations with Pump-system
  • Dark (i.e. brown) glass or UV resistant “covered” plastics containers
56
Q

Solution - SEVERAL SPECIAL FORMS

A

(direct intake, favourable taste)
• Elixir: clear, flavoured (high proportion of sucrose), alcohol (diluted ethanol or other polyhydric alcohols) and aromatic compounds (e.g. orange extract, cocoa, cinnamon)
• Syrup: concentrated, viscous aqueous solutions with high amount of sugars plus aromatic compounds
• Mixture: dispersed active ingredients in suitable liquid, less transparent, less amount of sugars, suspended solids may separate slowly

57
Q

Emulsion and Suspension - DEFINITION

A

Liquid preparations in which the active ingredient(s) is/are dispersed (suspended/emulsified) in a suitable liquid vehicle (dispersive phase)

  • In case of the emulsions the dispersed phase is liquid
  • In case of the suspensions the dispersed phase is solid
58
Q

Emulsion and Suspension - IMPORTANCES

A
  • During the storing/ on standing suspensions can get
    sediment - deposit formation
  • They have to be suitable for redispergation
  • Label/Sig. contains the terms ‘shake well before use’
59
Q

Emulsion and Suspension - USAGE

A
  • External: topical preparations (local or systemic)

- Internal: enteral, parenteral

60
Q

Emulsion - COMPOSITION

A
  • Active agent - Vehicles:
    *Distilled water or aqueous liquid, the active agent is fat-soluble, O/W (oil in water) type
    *Vegetable oils (corn oil, cottonseed oil, peanut oil, sesame oil), the active ingredient is water-soluble, W/O (water in oil) type
    -Auxiliary substances: the use of emulsifying (suspensifying) agents is required to minimize the surface tension existing between the two different phases
    O/W-type emulsifiers: soaps, sorbitan esters, PEGs
    W/O-type emulsifiers: wool fat, wool alcohol or stearin
61
Q

Emulsion and Suspension - CONTAINERS

A

Same as solutions:
- Vials, Glass, Bottle, Plastic flask
- Plastic tops or special closers, children resistant
closer (mainly for elixirs, syrups), multidose formulations with Pump-system
- Dark (i.e. brown) glass or UV resistant “covered” plastics containers

62
Q

Suspension - COMPOSITION

A

Dispersed powder in a liquid dispersive phase

63
Q

Injection and infusion - DEFINITION

A

Sterile liquid preparations are

  • Solutions
  • Emulsion or micro-emulsions
  • Suspension or micro-suspensions
64
Q

Injection and infusion - USAGE

A

intended for parenteral use

65
Q

Injection and infusion - Administration route

A

IV., IM., SC., IP., IC., IO, ID etc.

  • IV: oily solutions, NOT suspension/emulsion
  • Except micro-emulsions, micro-suspensions
66
Q

Difference bw. injection and infusion

A

Infusions are intended for slower or faster IV application

67
Q

Injection and infusion - SIGNIFICANCE

A
  • The effects of the enteral or parenteral applied drugs
    differ from one another (e.g. MgSO4)
  • Rapid effect is required (shorter absorption half-life)
  • Compound irritates the mucous membranes of GI
  • The stomach (i.e. low pH, enzymes) decomposes the
    drug
  • The oral treatment is impossible (because of injuries or
    the patient is unconscious /comatose/)
  • The drugs should not pass through the liver first
68
Q

Injection and infusion - CONTAINERS

A
  • Human injections and veterinary single dose formulations (in vials, less than 10 ml)
  • Veterinary multidose formulations (10-100< ml) in sterile glass bottles, closed with rubber-stoppers
  • Infusions (100-1000 ml) are dispensed in glass bottles, plastic bags
69
Q

Extraction - DEFINITION

A
  • Traditionally prepared from one or more medicinal herbs
  • In case of non-watery and true extracts the active ingredient content is extracted by the pharmacists or
    manufacturers (industrial conditions)
  • Watery extract can be prepared by both pharmacist and
    owners
70
Q

Extraction - CLASSIFICATIONS

A
  1. Based on their solid matter content
  2. Based on their extracting agents
  3. Based on principles of procedures
71
Q

Extraction - solid matter content

A
  • Liquid extraction (at least 50% extracted liquid material)
  • Semi-liquid extraction: solid matter content is bw 50-70%
  • Semi-solid extraction: solid matter content is bw 70-80%
  • Solid extraction degree of humidity: maximum 6%
  • Preparation, reconstitution of solutions
  • Can be used as sweetening or flavouring agents
72
Q

Extraction - their extracting agents

A

a) Watery /Aqueous/ extraction:
* Decoction (ingredients are extracted by cooking)
* Infusion (soaking in hot water)
* Extraction (soaking in tepid - lukewarm - water)
* Applied: Externally (rinsing and cleansing of surfaces), Orally or Inhaling
b) Alcoholic extraction; tinctures
- Adm: Externally (use on body surface or wounds)or Orally (mainly as appetizers)
c) Ethereal extraction
d) or other organic solvents (heptanes)

73
Q

Extraction - principles of procedures

A

Soaking, wet steaming, percolation (permanent flow of extracting agent through the percolator)

74
Q

Extraction - CONTAINERS

A

Tinctures are daylight sensitive

75
Q

Liniment - Definition

A

Thick, lotion-consistency dosage form for topical administration.

76
Q

Liniment - Usage

A

– Rare
– Skin diseases, rheumatism
– Horses: soreness, stiffness, cooling (alcohol+volatile oils)

77
Q

Liniment - Prescription

A 
– Official preparations (White liniment BP)
– Prepared preparations (rare)
– Licensed: infrequent (GSL, P)
*animal health care products
- ”Only for external use”
78
Q

Gaseous dosage forms

A 
For inhalation:
• Gases (N2O)
• Aerosols – For inhalation
For other:
• Aerosols – For topical use
• Foams
• Impregnated/Smoking strips
79
Q

Aerosols - DEFINITION

A

Aerosols (sprays) are based on solids (fine powders) or
liquids
- Delivered in the form of an aerosol
(appropriate valve or a suitable atomising device)
- The sizes of particles have to be smaller than 5 µm

80
Q

Aerosols - USAGE

A
  • External use: Treatment of skin and mucous membrane surface
  • Internal use: Intrapulmonary, via inhalation
81
Q

Aerosols - COMPOSITION

A
  • Active agents: disinfectants, AB, antifungals, parasiticides and anti-inflam agents
  • Vehicles (i.e. solvents): distilled water, diluted alcohol,
    propylene glycol etc.
  • Propellant gases: propane-butane, compressed air
    -Pressurised form (pressure is app. 250 kPa)
    -Non-pressurised form (suitable pump-system and dispersing)
82
Q

Aerosols - CONTAINERS

A
  • Sprays should be supplied in well-closed containers

- No opening or burning of the empty pressurised containers is allowed because of the risk of accident

83
Q

Impregnated/Smoking strips - Definition:

A

• Dosage forms intended for antiparasitic treatments of honey bees.
• Impregnated strips: put in the bee-hive check
the effect after 24 h
• Smoking strip: ignition–> put in the bee-hive in smoking state –> check the effect after 24 h
• The expelled mites should be burnt.

84
Q

Impregnated/Smoking strips - Prescribing

A

• Licensed

85
Q

Impregnated/Smoking strips - Example

A

E.g. Bayvarol impregnated strip

86
Q

Stability

A

In the given storage time interval the difference of the measured and the declared physical and chemical parameters′ values must be not greater than ± 5-10%

87
Q

Determinant factors of stability

A

a) Physical factors:
• Homogeneity (macroscopic, microscopic): description to a homogeneous drug preparation
• Emulsion stability
b) Chemical factors:
• Decomposition of the active substance
• Interactions: other active substances, vehicle, package material
• Environmental effects: air, light, temp, humidity

88
Q

Stability tests types

A

• Long term: 25°C, 60% RH: 0, 3, 6, 9, 12, 18, 24 and 36 months
• Accelerated: 40°C, 75% RH: 0, 3 and 6 months
• In use:
– Medicated drinking water: 0, 6, 12 and 24 hours
– Medicated feeds: 0, 1, 2 and 3 months
– Opened package: 0, 2 and 4 weeks
– On going: 25°C, 60% RH: 0, 3, 6, 9 and 12 months

89
Q

Measured parameters of stability tests

A 
– Content of active substances
– Concentrations of impurities
– Homogeneity: macroscopic, microscopic (particle size)
– Microbiological tests: e.g. sterility
– Density
– Viscosity
– pH
90
Q

Colloid chemical classification of drug formulations

A

INCOHERENT FORMULATIONS:
a) Heterogeneous>500nm: powders, emulsion,
suspension, granules
b) Colloidal (1-500 nm): colloidal solution, some stock
solutions
c) Homogenous (<1 nm): solutions, tinctures

COHERENT FORMULATIONS:
a) Heterogeneous: ointment, pastes, creams, tablets,
suppositories
b) Colloidal: gels

91
Q

Stability of emulsion

A
  • Phase separation
  • Phase inversion
  • Aggregation processes
92
Q

Pharmaceutical ingredients for suspension preparation

A

• Solubilizing agents: Polysorbate 20, 60, 80, Sodium lauryl sulfate
• Viscosity increasing agent: HEC, HPC, Silica colloidal anhydrous/hydrated
• Microbiological conservants/preservatives: Sorbic acid,
Preservative solution
• Other ingredients: Flavoring agents

93
Q

Terpineol containing suspension (Expectorant)

A

• In mortar the pulverized terpineol (Terpinum) should be
mixed thoroughly and gradually with portions of HEC
(Mucilago hydroxyaethylcellulosum).
• The suspension should be diluted with purified water, then it should be transferred to the bottle with given portion of water.
• Preservative solution (Solutio conservans) and peppermint stock solution (Diluendum menthae) should
be added and the liquid should be mixed thoroughly.

94
Q

Terpineol containing suspension: LABELLING

A
  • Internally, shake it well before use
  • Storage: 1 months, store at low temperature
  • Th: Expectorant
95
Q

Semisolid preparations:
• OINTMENT
• CREAM

A
  • OINTMENT - an ointment consists of a single-phase base in which solids or liquids may be dispersed.
  • CREAM: multiphase preparations consisting of a lipophilic phase and an aqueous phase
96
Q

Antirheumatic ointment - LABELLING

A
  • Externally. Keep in cold place.

Th: Antirheumaticum. Rubefaciens.

97
Q

Moisturizing cream - LABELLING

A

Externally. Keep in cold place.

Th: Moisturizer.

Pharmacology 1+2 (25 decks)

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