Intramuscular injections

Progesterone. Progesterone (1) is not orally active. Although seldom used clinically, it can be adrninistered as an intramuscular injection, pessaries, or suppositories in the treatment of menstmal disorders and habitual abortion (121). Progesterone can be recrystaUized from dilute alcohol and exists in two crystalline forms (122). It is soluble in chloroform and ethanol sparingly soluble in acetone, dioxane, ether, and fixed oils and practically insoluble in water (121). Two syntheses of progesterone (1) are described in Figure 3. 

Prolonged Action Parenterals Injections. Intramuscular injections have been developed to achieve prolonged therapeutic effects. This can be accompHshed by suspension of dmg particles in oils or flowable gels, from which the dmg slowly diffuses. Aqueous suspensions can also provide such therapeutic response. In these cases, the soHd dmg crystals generally are quite water insoluble and of a controlled particle size and crystallized form. 

The relative toxicities of thallium compounds depend on their solubHities and valence states. Soluble univalent thallium compounds, eg, thaHous sulfate, acetate, and carbonate, are especiaHy toxic. They are rapidly and completely absorbed from the gastrointestinal tract, skin peritoneal cavity, and sites of subcutaneous and intramuscular injection. Tb allium is also rapidly absorbed from the mucous membranes of the respiratory tract, mouth, and lungs foHowing inhalation of soluble thallium salts. Insoluble compounds, eg, thaHous sulfide and iodide, are poorly absorbed by any route and are less toxic. 

Meglumine [6284-40-8] antimonate [133-51 -7] C H NO HO Sb, (Glucantime) is a pentavalent antimonial used for the treatment of leishmania sis in Latin America (207) and in the French-speaking areas of Europe and Africa (206). It is adrxiinistered by deep intramuscular injection. Although relatively safe and usually well tolerated, numerous side effects have been observed. It is not available in the United States. 

Progestin-only contraceptives (Fig. 4) contain low-doses of progestins (e.g. 350 pg norethindrone or 75 pg norgestrel) that have to be administered daily without interruption. The lowest expected failure rate during the first year of use is 0.5%, while the typical failure rate amounts to 3%. Subdermal implants of norgestrel (216 mg) for sustained release provides for long-term (for up to 5 years) contraceptive effects characterized by failure rates of only 0.05%. Reliable contraception for 3 months can be achieved by an intramuscular injection of a crystalline suspension of 150 mg medroxyprogesterone acetate (Fig. 3) (failure rate 0.3%). 

Historically the only melanocortin peptide to be used clinically is the parent hormone from which all these peptides are derived from namely ACTH (see above). It has also been used in the treatment infantile spasms for epilepsy, where it is administered as an intramuscular injection only over a 2-12 weeks period. Obvious side effects include weight gain, puffy face, high blood pressure and an increased risk of infection and should never be administered to patients with diabetics, renal or heart failure. ACTH is also used as a stimulation test to measure adrenal cortex activity, i.e. production of cortisol and is used to ascertain whether someone has Addison s disease. 

Epinephrine (adrenalin) 0.1 to 0.5 mg may be given by subcutaneous or intramuscular injection. Hypotension and shock may be treated with fluids and vasopressors. Bronchodilators are given to relax the smooth muscles of the bronchial tubes. Antihistamines may be given to block the effects of histamine. 

A subcutaneous (SC) injection places the drug into the tissues between the skin and the muscle (see Fig. 2-5B). Drug administered in this manner are absorbed more slowly than are intramuscular injections. Heparin and insulin are two drug most commonly given by the SC route... 

Although the drug is most often administered orally, warfarin injection may be used as an alternative route for patients who are unable to receive oral drag. The intravenous dosage is the same as that for the oral drug. Intravenous warfarin is administered as a slow bolus injection during a period of 1 to 2 minutes. Warfarin is not recommended for intramuscular injection. After the drug is reconstituted, it is stable for 4 hours at room temperature. The vial is not recommended for multiple use, and any unused solution should be discarded. 

The well-known adverse reaction formerly often observed after intramuscular injection of clemizol penicilUn in the treatment of syphilis with anaphylaxis-like symptoms plus CNS involvement in the absence of immimological sensitization to penicillin was called the Hoigne syndrome or embolic-toxic reaction, and might be explained by intravasal appUcation of LA with subsequent toxic effects [8]. 

In anaphylaxis, epinephrine appears to have an optimal benefit-to-risk ratio when it is administered promptly by intramuscular injection [1-6]. 

It is not surprising that intramuscular injection of epinephrine into the vastus lateralis produces a prompt peak plasma epinephrine concentration, because of the large size and excellent vascularization of this muscle. It is also not surprising that subcutaneous injection of epinephrine potentially leads to delayed absorption, because of the potent Ui-adrenergic agonist vasoconstrictor effects in the skin and subcutaneous tissue, as evidenced by skin blanching at the injection site [19, 20]. 

Simons PER, Lieberman PL, Read EJ Jr. Edwards ES Hazards of unintentional injection of epinephrine from auto-injectors a systematic review. Ann Allergy Clin Immunol 2009 102 267-272. Rawas-Qalaji MM, Simons PER, Simons KJ Sublingual epinephrine tablets versus intramuscular injection of epinephrine dose equivalence for potential treatment of anaphylaxis. J Allergy Clin Immunol 2006 117 398-403. 

Teicoplanin is a naturally occurring complex of five closely related tetracyclic molecules. Its mode of action and spectrum of activity are essentially similar to vancomycin, although it might be less active a inst some strains of coagulase-negative staphylococci. Teicoplanin can be administered by intramuscular injection. 

Polyclonal Antibodies against FORL r purified polygalacturonase were raised in white rabbits. For the first immunization 200 jxg of purified protein in 300 jxl of distilled water was mixed with 200 1 of PBS and 500 n of complete Freund s adjuvcmt and injected intramusculary into the leg. Two subsequent intramuscular injections, each containing 300 fig of protein in 1 ml of incomplete Freund s adjuvant were given at 1 month intervals. Finally, the rabbit was bled 1 week later. The antisera, separated from blood by incubation at 37 "C, were stored in 1 ml fractions at -20 C. 

Opioids maybe administered in a variety of routes including oral (tablet and liquid), sublingual, rectal, transdermal, transmucosal, intravenous, subcutaneous, and intraspinal. While the oral and transdermal routes are most common, the method of administration is based on patient needs (severity of pain) and characteristics (swallowing difficulty and preference). Oral opioids have an onset of effect of 45 minutes, so intravenous or subcutaneous administration maybe preferred if more rapid relief is desired. Intramuscular injections are not recommended because of pain at the injection site and wide fluctuations in drug absorption and peak plasma concentrations achieved. More invasive routes of administration such as PCA and intraspinal (epidural and intrathecal) are primarily used postoperatively, but may also be used in refractory chronic pain situations. PCA delivers a self-administered dose via an infusion pump with a preprogrammed dose, minimum dosing interval, and maximum hourly dose. Morphine, fentanyl, and hydromorphone are commonly administered via PCA pumps by the intravenous route, but less frequently by the subcutaneous or epidural route. 

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