1. Karel Urbánek Ústav farmakologie LF UP a FN Olomouc
Parenteral drug forms
Karel Urbánek
Ústav farmakologie LF UP a FN Olomouc

2. Parenteral drug forms
Intended for administration by injection, infusion, or implantation
Must be sterile and apyrogenic

3. Parenteral Drug Forms Injections Infusion
different volume, composition, use
vater for injection (aqua pro iniectione),
oil for injection (oleum pro iniectione)
Implants

4. By route of administration
Intravenous (i.v.)
Only water based solutions (or very fine emulsions)
Immediate and precise blood levels
Irritating substances
Bolus or drip infusion

5. By route of administration
Intramuscular (i.m.)
- Solutions, emulsions and suspensions
Maximal volume 5 ml
Reservoir with different speed of absorption
based on its chemical and physical properties
based on the condition and properties of the muscle

6. By route of administration
Subcutanneous (s.c.)
Under the skin, fast absorption via blood and lymph
Solutions and suspension up to 2 ml
Absorption can be slowed down suspension or vasoconstriction
implants

7. Infusions - glass

8. Infusions - plastic

9. Infusions - plastic

10. Infusion set

11. All-in-One

12. Pump

13. Continual injection
Linear dosing pump

14. Main infusion solutions
electrolytes
sugars
aminoacids
fats
crystaloids and colloids

15. Crystaloids Water and electrolytes Pass freely across membranes
Low volume efficiency
Non-balanced
= mostly only Na + Cl
Dilution acidosis
Hyperchloremic acidosis
Balanced
= contain Ca, K, Mg + lactate or bicarbonate

16. Crystaloids Normal saline isotonic (0.9%) solution of NaCl,
(Natrii chloridi infusio 0,9%)
used as carrier solution for parenteral drugs, or to replace loss of sodium
obsolete
non-balanced

17. Crystaloids Hartmann (Hartmanni infusio, H1/1)
for correction of loss of fluids and electrolytes (burns, trauma, hypovolemic shock). Contains lactate which has alkalifying properties
Darrow (Darrowi infusio, D1/1)
Has more potassiums

18. Crystaloids Ringer (Ringeri infusio, R 1/1)
used in mild metabolic alkalosis, in loss of water and sodium or as carrier solution
“Half” solutions (F1/2, R 1/2)
mixed with 5% G

19. Crystaloids Balanced solutions - similar to plasma composition
- minimal potential base excess
- always preferred when giving large volumes
Plasmalyte
Na+ 140; K+ 5,0; Mg2+ 1.5; Cl- 98; acetate 27; gluconate 23 mmol/l
Ringerfundin
Na+ 140; K+ 4.0; Mg2+ 1.0; Ca2+ 2.5; Cl- 127; acetate 24; malate 5.0 mmol/l

20. Volume efficacy

21. Volume expansion

22. Colloids
Intended for supplementation and maintenance of intravascular volume
Always with crystaloids! (usually 1:4)
First use in WWI
1963 Thompson and Walton - hydroxyethylstarch
Nowadays – albumin, gelatine, dextran, HES

23. Hydroxyethylstarch Volume-expanding solution (plasma expander)
Solutions of 6% and 10%
6% - isooncotic – you get as much as you give
10% - you get 1.5x as much

24. Hydroxyethylstarch Adverse effects Bleeding
complex with F VIII and fibrinogen
Anti platelet effect

25. Hydroxyethylstarch Adverse effects Anaphylactoid reaction
direct mastocyte and basophil stimulation
incidence 1:1200 (14 / cases)*
approx. 8x higher than albumin
* Ring J, Messmer K. Lancet 1977; 1:466-9

26. Hydroxyethylstarch Adverse effects Serum amylase elevation
not a sign of pancreas irritation
decreased renal elimination of HES + AMS
up to 72h (up to 5 days non-diagnostic)
* Kohler et al. Int J Clin Pharmacol 1977; 15:428-31

27. Hydroxyethylstarch Adverse effects Pruritus
cumulation in MoMa system in the skin
not caused by histamin release
dose dependent (?)
onset in 1 – 6 weeks
lasts for 9 – 15 weeks
antihistamines without effect

28. Hydroxyethylstarch
Brand names
HAES Steril
Hemohes
Voluven
Tetraspan

29. Gelatine (Gelatina succinata)
Dextran

30. Human albumin (Albuminum humanum)
20% solution of albumin is hyperoncotic, has plasma expanding and anti-edema effects
5% solution of albumin is isooncotic
Indications
rarely for hypovolemia (price, risk of infection)
hypoalbuminemia in burns, liver failure and cirrhosis, nephritis, nephrotic syndrome, GIT disorders, Lyell syndrome, ascites,...

31. Acid Base Balance corrections
Acidosis
Infusio natrii hydrogenocarbonatis 8.4%
1000 mmol of sodium bicarbonate in 1000 ml
NaHCO3 (mmol) = b.w. (kg) x 0.3 x base deficit (mmol/l)
usually only give half of the calculated dose!
Alkalosis
Argininechlorid 21%

32. Ion dysbalance corrections
Hypokalemia
less severe – tablets with KCl
severe – 7.5% solution of KCl i.v.
Injectio kalii chloridi 7.5%
10 ml injections
always dilute in saline – 2 inj into 500 ml