Pract 5, 6, 7 Flashcards
Solution:
- System: Homogenous disperse
- Solvent: liquid
- Solute: Solid/gas/liquid
- Precipitate: No, clear
Emulsion:
- System: heterogenous dusperse (o/w, w/o)
- Solvent: liquid
- Solute: liquid
- Precipitate: yes, liquid
bigger than 500nm = NEVER IV
Suspension:
- System: heterogenous disperse
- solvent: liquid
- solute: solid
- precipitate: yes, solid
bigger than 500nm = NEVER IV
Microemulsion/microsuspension:
very small -> can be used IV
Microemulsion:
- propofol
- microlipid infusion (used when they cant eat)
Microsuspension:
- Fenbendazole and Flubendazole = antiparasitic agent. Fine powderm miced in water.
W/O and O/W systems:
- Weaper O: w/o = oil is the largest phase. water in oil
- Oper W: o/w = water is the largest phase. Oil dissolved in water
Injection vs Infusion
both: Liquid - parenteral
Injection (injectio):
- solution, Emulsion, Suspension, Microemulsion, Microsuspension
- smaller than 100ml
Infusion (infusio):
- solution, microemulsion
- More than 500ml
can be given SC
Injection, infusion - requirements:
Requirement for all:
- sterile
- pyrogen-free (pyrogen = fever)
- isotonic
- isohydric (pH between 5 and 7)
+ homogenous, particle free (solution)
Liquids for Oral and Rectal use:
- solution
- emulsion
- suspension
- syrup (sirups): better taste, much sugar. not frequently used in Vet.med
- Elixir, mixture: have alcohol content. Do not give in case of liver failure
- Extract (extractum, Tinctura): can be dry, water and alcoholic. Substract substances from herbal parts. Do not give to liver failure patients!
- Drop for oral use (Gutta): when you only need a small dose. Not frequently used.
Liquid for skin, mucous membrane:
- solution
- emulsion
- suspension
- spot on/ pour on
- shampoo
- teat dip solution
- extract
- inrauterin solution, suspension
Liquid for ophthalmology:
- solution, suspension
- sterile!
- active agent (AB, GC, NSAID, emetics, drug acting on autonomous NS)
- vehicle: same as binders, give volume (Water, castor oil, but sterile!)
- preservative (benzalkonium chloride)
- expiration date: quicker when you open it, only for four weeks.
Difference between Steriods and NSAIDS in ophthalmology:
Steroid:
- glucocorticoids
= causes immune suppression, so never use incase of viral infections
= decrease the healing of cornea
= use flourossence test –> turns green in case of damage
Liquid for - Otology, nasal cavity
- Ear cleaner: contain detergent and antiseptic agent to remove the discharge
- Ear drop (otogutta):
- solution, suspension
- active agent (AB, antifungal, GC, antiparasitic…)
- vehicle (water, alcohol, propylene glycol…)
- Malassezia pachydermatitis: yeast fungi in otitis externa
- Pseudomonas aeroginosa: bacteria in otitis externa - Nasal drop (nasogutta): BbPi
- nasal spray
Semi-solid:
- field of application and dose form:
- Skin, mucous membrane:
- Ointment (unguentum), Cream (cremor), Gel (gelum) - Oral:
- Gel (gelum), Paste (pasta), Electuaries (Electuarium) - Eye:
- Eye ointment (Oculentum) - Mammary gland:
- Intraammary infusion - Rectum, Vagina:
- Suppository (suppositorium), Vaginal suppository (Ovulum)
Semi-solid:
- properties
- active agent - various
- homogenous appearance:
- body temp does not melt it
- local or systemic effect
Semi-solid ointment Active compounds:
- Antibiotics, antimycotic, antiviral agents.
- NSAIDS, glucocorticoids, antihistamine
- coating, antiseptic agents
Semi-solid ingredients:
VEHICLE:
Lipophilic:
- fats and oils: cocoa butter, oils (sunflower, eanut, castor, cod liver oil), hard fat
- hydrocarbons: vaseline and paraffins
- Waxes and wax alcohols: wool wax (Lanolin), honey bee wax, cetostearyl alcohol
= can not wash it with water, longer duration than hydrophilic
Hydrophilic:
- natural polymers: cellulose, gelatine, starch
- syntehtic polimers: macrogols (polyxyethylenes), and polysorbates (tween).
Semi-solid ointment w/o:
can not be washed with water
- hydrous ointment
- emollient ointment
- (simple ointment)
- (oily ointment)
Semi-solid ointment o/w:
- nonionic hydrophilic ointment
- anionic hydrophilic ointment
- (noniunic emulsifying ointment)
- (anionic emusifyying ointment)
Semi-solid:
cream, gel
Cream:
- emuslion system
- hydrophilic o/w
–> emulsifiers: Na-soap, Polysorbate
- lipophilic w/o
–> emuslifiers: Wool wax alcohol
Gel:
- gellifying agent: starch, cellulose, colloid SiO2
Semi-solid - eye ointment:
- active agent, Vehicle
Active agent:
- AB, GC…. same as eye drops
Vehicle:
- opthalmic white vaseline
- simple eye ointment
- hydrous eye ointment
= like the ointment, but always sterile!
= they always need to have eye or the opthalmic word in them
- sterile!
- longer duration of action than eye drops!
Semi-solid - intramammary infusion
- properties
- sterile
- soft suspension, emulsion
- prevention, treatment
- lactating (Lactating Cow (LC) repeat in 12 hours, Milking Cow (MC))
- dry cow (DC): will stay there for a longer period. To preent infection. Lower WP than LC and MC.
- difference in ingredients: DC = Bismuth salts (closes the teat canal)
Semi-solid - intramammary infusion
- composition
- Active Agents:
- AB, GC, enzymes, antioxidants
- bismuth salts - Vehicle:
- liquid paraffin
- white vaseline
- medium chain triglycerides
Semi-solid - intramammary infusion
- application:
- udder wash
- disinfection (chlorhexidin used as antiseptic)
- milk out
- infusion through the teat channel (1syringe/teat)
- a) lactating –> milk out again after 12 hr, than repeat
- b) Dry –> last milk out (WP)
Semi-solid - suppository:
- properties, active agent, vehicle
Rectum and vagina
Properties:
- Body temp: softening –> melting
- Local (eg. obstipation) and systemic (eg. diazepam) effect
Active agent:
- anticonvulsive, antipyretic, painkiller
- faecal softener, antiseptic
Base/vehicle:
- solid fat
- cocoa butter
Semi-solid - electuraries
- properties (ative agent, vehicle):
= a powder you mic to something tasty so the animal will eat it. Orally. Not authorised, you mix it yourself
Active agent: weak! <– imprecise
Active agent: solid (powder)
Vehicle:
- syrup, molasses, jam
Gaseous
- classification by usage
- inhalational (inhalanda - gas)
- external (skin, mucous membrane - foam, spray)
- Environment (foam, spray, gas)
- Teat spray
- Impregnated-, smoking strip (honey bee)
- Vagina, rectum - foam, spray
Gaseous - inhalational
- Base and container:
Base:
- Gas (N2O, O2): should always be combined with other anastetic agents
- Liquid: evaporates
- isoflurane, sevoflurane
- GC - fluticasone, beclomethazone: asthma
- B2 agonist - terbutaline, formoterol, salmeterol : bronchodilation in ling asthma - Solid: human
Container:
- compressed gas
- propellant
- mechanical
Gaseous - impregnated, smoking strips:
treatment of honey bees.
Impregnated strip (smoking strip): into the bee hive. Smoke contain the A.S need to be lighted
- honey bees, external parasites (Varroa destructor) - mites
1. Volatile oil: - thymol, caphor, menthol, eucaplyptus
- safer agents - good
2. Formic acid, oxalic acid: - sage agents - natural products
3. Amitraz: - not natural - more dangerous. Acts agains all arthropods, also the bees
4. Flumethrin: used in pyrethroid. parasitic agent, repellent effect - not natural - more dangerous. Acts agains all arthropods, also the bees
5. Coumaphos: organo sulphate, also used for nerve gas in boar - not natural - more dangerous. Acts agains all arthropods, also the bees
Colloid chemical classigication of drug formulations:
Incoherent formulations:
- Heterogenous (>500nm): powders, emulsion, suspension, granules.
- Colloidal (1-500nm): colloidal solution, some stock solution
- Homogenous (<1nm): solutions, tinctures
Coherent formulations: (water included)
- Heterogenous: oiintment, pastes, creams, tablets, suppositories
- Colloidal: gels
Liquid drug formulations-emulsions definition:
- liquid preparations in which the active ingredient(s) is/are dispersed (emulsified) in a suitable liquid vehicle (disperive phase)
- in case of the emulsion the dispersed phase is liquid
Liquid drug formulations-suspension definition:
active preparation in which the active ingredient(s)
- is/are dispersed (suspended) in a suitable liquid behicle (dispersive phase)
- in case of the suspension the dispersed phase is solid
Semisolid preparations-ointments and creams definitions:
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 a aqueous phase
Washability of ointment bases:
- steps to be taken
- cover the surface of the slide with the selected ointment base
- put it into the beaker (45*C) and add water drops to it (20 ml/min, total 50ml)
- measure the size of the surface remained without ointment base
Based on this assya you can detect:
- hydrocarbon ointment bases (applied in case of skin irritative agents or for coating effects
- emulsion-type w/o or o/w cream
- hydrogels/macrogol ointment
Moisturizing cream:
- method
- heat the ointment base to around 70*C
- add the heated mixture of glycerol, sodium lauryl sulphate and purified water to the melted mixture of microcrystalline paraffin, liquid paraffin and cetosearylalcohol under continous stirring.
- stir the cream until it cools then add purified water to reach the final mass.
- add lemon oil and mix it at once
- labelling: externally. keep in a cold place.
Suppositories:
- method
- wipe the casting moulds with the liquid paraffin and put them into the refrigerator (+5*C)
- heat the base hard fat until it gets opalescent
- add the active ingredient to the base while you are stirring it
- pour it into the casting mould
- put the matric back to the refrigerator
- when the suppositories are firm they can be taken out from their moulds and wrapped one by one
- package and labelling
The aim of enteric coating in capsules:
- protection of active substanve or gastric mucosa
- intestine targeted therapy
- acid liable drugs: erythromycin, omeprazol, enzymes…
Common pH-sensitive polymers used in drug delivery:
- aminoalkyl meethacrylate copolymer (Eudragit E)
- Poly (methacrylic acid-co-methyl methacrylate) (Eudragit L/S)
- Hydroxypropyl-methylcellulose phthalate (HPMC-P)
Functions of ingredients in capsules:
- Resin: shellac
- Polymer: alginate, CAP, RVAP, HPMC, EC, HPC
- plasticizer: triethyl citrate
- Preservative: sorbates
- Lubricant: plamitic acid
- Sweetner: sucrose, honey
- Opacifier: titanium oxide
Antiulcer drugs:
- Antiacids
- inhibition of acid secretion:
- H2-antagonist
- proton-pump inhibitors –> the effect is prolonged because you need to wait for the revirsible effect - Enhancer of mucous membrane:
- PGE-analogs
- Sucralfat
- Bizmuth salts
Proton-pump inhibitors (PPI):
Omeprazole, Pantoprazole
Pharmakokinetics:
- acid sensitive –> capsules, coated tablets. 30min before meal
- effect: 2-6 hr (IV. slow)
- Accumulation in parietal cells (max effect after 3-4 days) –> prolonged
Doses:
- 0.71.5 mg/kg SID oral (Ca, Fe)
- 4 mg/kg SID oral (eq)
- WP: gradual after 3-4 weeks (rebound)
- Dysbacteriosis -> probiotics
Good Manufacturing Practice (GMP):
GMP requires that medicines:
- are of consistent high quality
- are appropriate for their intended use
- meet the requirements of the marketing authroisation or clinical trial authorisation
The environmental conditions, maufacturing process, procedures, materials, etc… have to be controlled even in- process and well-dokumeted.
Harmonisation of GMP ativites at Europen Uniun level: EMA
Routes of administration:
External: mostly local effect (except spot on, pour on and fentanyl patch)
- Skin, mucous membrane
- ear, eye, nose
Internal: mainly systemic effect
- Enteral: oral + tube, rectal
- Parenteral: SC, IM, IV, IP, IA, IO, IC, ID.
- Other: udder, airways, uterus, vagina
Horse:
- Routes of administration, characterization
- Medicated feed:
- disadvantage: nor sure about the exact amount consumed
- needs to have huge TI! - Orogastric tube:
- more presise
- activated charcoal in toxaemia.
- they dont want to swallow it, therefore this is a good method - Gel/paste:
- nice flavour; carrot, apple
- chewable tabl. - IV injection:
- mostly used - IM injection:
- Often lead to an abscess - Intrauterine tablet:
- not frequent, they dont tolerate it
NO SC!
Ruminants
- Routes of administration, characterization
- Oral (feed, water, drench):
- you can not give AB orally to a Ru, because it will kill all the microbes. Only to calves less than 2 months
- drench: gives the same amount every time. good for a big herd - Intraruminal device:
- deworming.
- long prolongation. Long WP - Pour on
- Intrauterine tabl
- Intravagina drug delivery system
- intramammary infusion
- IV injection: V.jugularis
- IM injection: neck + butt
- SC injection: neck + behind the ears
- Spray (like swine)
Swine
- Routes of administration, characterization
Mostly mass medication! - except in valuable breeder animal
- Oral (feed, water, drench)
- IM injection: neck + butt.
- neck mostly used, less valuable meat - SC injection: skin behind ears
- Spray:
- external. Local AB or antiparasitic - Nasal drop (notril):
- used in piglets in small amounts when they can not open their mouth. they will swallow it
NO IV! can be given in V.auricularis, but not frequent
Poultry:
- Routes of administration, characterization
- M. feed: most common
- they can see it in the feed, and select it out - M. drinking water: most common
- most preferred!
- they will more likely drink if they are sick rather than eat - Tube: not frequent
- Spraying: AB or antiparasitic
- IM injection: pectorals
- SC injection: Skin of the neck
- Fumigation/vapours: used for vaccination in farms. inhalation
8: IV. vein under the wing. not frequent
Drug administration to farm aninals on a large scale:
- external
Without fixation:
- dustbag, dusting gate (antiparasitic)
- Footbath: RU. Antiseptic agents ZnSO4, CuSO4.
- sprayin
With fixation:
- Dipping (remember sheep!) AS: amitraz diaziron.
- pour on
- impregnated ear tag
Drug administration to farm animals on a large scale:
- Internal
Without fixation:
- medicated feed
- medicated drniking water
- salty blocks
With fixation:
- drench
- mass vaccination
- fumigation, vapours (fogger)