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[Results of intramuscular injection of glycosamino-glycanpolysulfate (GAGPS) in experimental arthrosis of the knee in dogs (author's transl)].

Report on the action of GAGPS injected intramuscularly on experimental arthrosis of the knee-joint in dogs. In both hind-legs the lateral tibial joint-surface and the lateral meniscus were resected. This produces arthrotic changes similar to human arthrosis within 2 months. Of 27 dogs 13 received i.m. injections into the glutei of GAGPS (25 mg/kg). 14 dogs were not untreated controls. After the 7th postoperative day the injections were given on every third day on 10 occasions, thereafter every fourth day for another 10 occasions. The animals were killed 3 months after the start of the experiment. Loss of cartilage on the lateral condyle proved to be clearly less pronounced in the treated animals than in the controls, macroscopically, radiologically and histolocally. GAGPS, injected, intragluteally, limits loss of cartilage in experimental arthrosis of the knee in dogs.

Animals

Treatment of cystic ovarian disease in dairy cattle. Comparative observation of the effects of an intramuscular injection of corticosteroids and an intravenous injection of a combination of human chorionic gonadotropin and progesterone.

Of 67 cows with cystic ovarian disease (COD), 34 were injected intramuscularly with 20 mg of betamethasone of 10 mg of dexamethasone (CC) and 33 intravenously with a combination of 3,000 IU of human chorionic gonadotropin and 125 mg of progesterone (HCG -P). Pregnancy rates and intervals between treatment and conception were 32.4% and 32.1 +/- 30.5 days, respectively, in the CC-treated cows and 30.3% and 51.6 +/- 29.5 days in the HCG -P-treated ones. Cows which had not responded to gonadotropin treatment showed a considerably higher pregnancy rate when treated with CC and a lower pregnancy rate when administered with HCG -P than those which had received no treatment before. There was a trend that the earlier a cow was treated, the more readily she recovered. CC injection gave a satisfactory result even when performed long after calving. The estrous behaviour seemed to be related with prognosis in cows with COD. In both CC-treated and HCG -P-treated cows, the pregnancy rate was the highest in cows showing anestrus and the lowest in those exhibiting irregular estrus.

Animals

Changes in plasma enzyme concentrations following intramuscular injections and gastroscopy.

The effects of intramuscular injections on plasma creatine kinase (CK), aspartate amino-transferase, lactate dehydrogenase, and hydroxybutyrate dehydrogenase concentrations were examined in 19 patients given intramuscular premedication for gastroscopy, and 18 patients given other intramuscular injections. Only CK concentrations showed significant increases which were as high as four times the upper limit of normal, and affected a maximum of 51% of patients at 12 hours after the first injection. Elevated CK concentrations persisted for up to 72 hours, and followed injections of diazepam, various antibiotics, and the combination of a narcotic analgesic with atropine. Gastroscopy did not appear to increase plasma enzyme concentrations in six patients who were given intravenous premedication. The significance of these findings to the diagnosis of myocardial infarction is discussed.

Adult

Subcutaneous infusion and intramuscular injection of desferrioxamine in patients with transfusional iron overload.

The effects of intramuscular injection and subcutaneous infusion of desferrioxamine (D.F.) on urinary iron excretion were compared in eleven patients with thalassaemia major and one with congenital sideroblastic anaemia who were being maintained on regular blood-transfusions. Total (48-hour) urinary iron excretion ranged from 3-3 to 40-3 mg (mean 16-3 mg) in nine patients who received 750 mg D.F. intramuscularly before transfusion and from 3-9 to 32-3 mg (mean 11-9 mg) in ten patients who received D.F. by the same route after transfusion. In all 9 patients studied before transfusion, continuous subcutaneous infusion of 750 mg D.F. over 24 hours increased iron excretion by 61-5 to 135-8% (mean 101+/-25-4 S.D.%) compared with intramuscular injection of a similar dose. In the 10 patients studied after transfusion, the iron excretion produced by continuous subcutaneous infusion was from 18-9 to 213% (mean 128+/-74-3%) more than that produced by a single intramuscular injection of D.F. When the subcutaneous dose over 24 hours was increased to 1500 mg in six patients, 48-hour iron excretion ranged from 29-2 to 81-2 mg (mean 52-4 mg) and was increased by 80-2--794% (mean 429%) compared with the excretion when 750 mg was given by intramuscular injection. It is concluded that continuous subcutaneous infusion of D.F. produces more iron excretion in patients with iron overload than intramuscular injection. Providing a suitable portable pump can be carried by the patients, continuous subcutaneous infusion of desferrioxamine may prove a valuable means of preventing or treating iron overload in anaemic patients maintained on regular transfusions.

Adolescent

Effect of positioning on discomfort from intramuscular injections in the dorsogluteal site.

An intramuscular injection into a relaxed muscle is believed to result in less discomfort than an injection into a contracted muscle. When the femur is internally rotated, the gluteus maximus muscle is relaxed. The hypothesis that a dorsogluteal injection with the femur internally rotated will cause less discomfort than when the femur is externally rotated was tested in 44 surgical patients who received two injections of preoperative medication. Each patient received an injection of a narcotic medication and one of diazepam. All possible combinations of the factors--position (internal and external rotation), order of injection (first or second injection), and medication (narcotic or diazepam)--were determined, and patients were randomly assigned to one of these conditions. Patients rated their perceived discomfort after each injection on a five-point scale. The hypothesis was supported by discomfort ratings from injections of both types of medications, although diazepam injections caused significantly more discomfort than injections of narcotics. Older patients tended to report less discomfort from diazepam injections than younger patients. Sex, order of injection, and nurse administering the injection did not significantly influence discomfort ratings.

Adult

Intramuscular injections and bioavailability.

Bioavailability of drugs following intramuscular injection is reviewed, with particular emphasis on diazepam, chlordiazepoxide, phenytoin, digoxin and lidocaine. Clinical experience with these drugs has shown that i.m. absorption may be slow, erratic or incomplete. Factors which play a role in the bioavailability of i.m. medications include the water solubility of the drug, dispersion of the injected solution and blood flow at the muscle site. For many drugs, intravenous injection is the parenteral route of choice, and oral administration may be more efficacious than i.m. injection.

Absorption

Clinical pharmacokinetics of lorazepam. II. Intramuscular injection.

A single dose of 4 mg of lorazepam was injected into the deltoid muscles of six healthy male volunteers. Multiple venous blood samples were drawn during 48 hr after the dose and all urine was collected for 24 hr after the dose. Concentrations of lorazepam and its major metabolite, lorazepam glucuronide, were determined by electron-capture gas-liquid chromatography. Lorazepam was rapidly absorbed from the injection site, reaching peak concentrations within 3 hr. Mean pharmacokinetic pamrameters for unchanged lorazepam were: apparent absorption half-life: 21.2 min; elimination half-life: 13.6 hr; volume of distribution: 0.9 L/kg; total clearance: 58.2 ml/min. Lorazepam glucuronide rapidly appeared in plasma, reached peak concentrations within 12 hr of the dose, then was eliminated approximately in parallel with the parent drug. Within 24 hr a mean of 47.6% of the dose was recovered in the urine as lorazepam glucuronide and less than 0.5% was recovered as unchanged lorazepam.

Adult

Comparison of serum levels after intramuscular injections of 2% and 10% cis(Z)-flupentixol decanoate in Viscoleo to schizophrenic patients.

The serum concentrations of cis(Z)-flupentixol after injection of 2% and 10% cis(Z)-flupentixol decanoate in Viscoleo (Depixol injection, Fluanxol Depot) have been investigated in a crossover study with eight schizophrenic patients. No statistically significant difference was found between the two preparations when the data from individual days or areas under the serum concentration curves were considered. For the individual patients a difference was found between the two treatments in six cases; one preparation gave the higher serum concentration in four cases and the other preparation in two cases. Thus, the difference found within individual patients reflects the intraindividual variation rather than a difference between preparations. The maximum serum concentration was seen at 4 or 7 days after injection. The maximum/minimum fluctuation ratio indicates that dosage intervals longer than 2 weeks seem reasonable for most of the patients. The similarity in the serum concentrations, no matter which concentration of flupentixol decanoate solution was given, indicates that a dispersal and possibly a metabolic breakdown of the oil depot takes place in the muscle.

Adult

125I-labelled botulinum A neurotoxin: pharmacokinetics in cats after intramuscular injection.

1. On unilateral injection of sublethal doses of 125I-botulinum A neurotoxin (BTA) into one gastrocnemius muscle of the cat we found after 48 h: a) A disto-proximal gradient of radioactivity (RA) had developed in the sciatic nerve of the injected side. b) The ventral roots of the spinal cord half segments supplying the injected muscle showed a higher RA than the ventral roots of the contralateral control side. c) The spinal cord half segments innervating the injected muscle had a RA much higher than the corresponding segments of the contralateral side. However, a small rise of RA was also observed in the contralateral half segments. 2. In histoautoradiographs of the (ligatured) ventral roots the RA was strictly confined to the intraaxonal space of a few nerve fibres. 3. On injection of equal doses of 125I-BTA into either gastrocnemius muscle we found after 38 h: a) Direct stimulation of only one of the injected muscle caused the RA to reach a higher level in the spinal cord half segments ipsilateral to the stimulated muscle than in the spinal cord half segments of the non-stimulated side. b) Unilateral stimulation of one gastrocnemius nerve under the influence of gallamine or unilateral antidromic stimulation of the dorsal roots L7, S1 failed to cause a difference in RA between stimulated and non-stimulated side.

Animals

15(S)15-methyl prostaglandin F2alpha for termination of very early human pregnancy. A comparative study of a single intramuscular injection and vaginal suppositories.

The results of a comparative study of the efficacy and acceptability of 15(S)15-methyl prostaglandin F2alpha (15-Me-PGF2alpha) administered as a single i.m. injection or vaginal suppositories (15-Me-PGF2alpha methyl ester) every 3rd hr for termination of very early human pregnancy is reported. The amenorrhoic period varied from 37 to 60 days. Group I (30 cases) received 0.6 mg as a single i.m. injection without any pretreatment. Retrospectively 24 of the 30 women were in fact pregnant and 22 of them aborted. Group II received suppositories (1.0 or 1.5 mg per suppository). In this group all women were pregnant and they all aborted. Symptoms such as pain, bleeding, vomiting and diarrhea started in general earlier in the i.m. group and they were more marked. In the present series the efficacy and acceptability were highest for the vaginal route of administration.

Abortion, Induced