Concentration of Antibiotic and Chemotherapeutic Agents in the Ejaculum

Armstrong, Joseph R.; Cook, Ferris E.; Robison, Jack R.

doi:10.1016/s0022-5347(17)62477-7

Cited by 24 publications

(8 citation statements)

References 7 publications

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“…Early in 1947, Pulaski and Sprinz 26 attempted to measure streptomycin concentration in prostate slices from three deceased subjects and in the prostatic fluid from six living subjects treated with this drug, but with largely negative results. The investigation of the drug concentrations in the whole semen ejaculate can be tracked back to 1968 when Armstrong et al 27 reported that six antibiotics achieved higher concentration in semen, whereas the concentration of six other antibiotics was lower than that found in the serum of patients with prostatovesiculitis treated for 72 h. In 1975, Malmborg et al 28 used a qualitative split ejaculate technique along with a biochemical marker (zinc) to indicate that pivampicillin concentrations were higher in the first, zinc-rich, so-called ''prostatic'' fraction. This was based on a simplification of a quantitative method most fully developed by Lundquist in 1949, although Lundquist did not study the concentrations of drugs.…”

Section: Traditional Approaches To Study the Pharmacokinetics Of The mentioning

confidence: 99%

Male Genital Tract Pharmacology: Developments in Quantitative Methods to Better Understand a Complex Peripheral Compartment

Cao

2007

Clin Pharmacol Ther

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A substantial health burden results from medical problems affecting the male genital tract, including chronic morbidity conditions affecting a large proportion of men, such as benign prostatic hypertrophy and prostatitis, and potentially lethal conditions, such as prostate cancer and human immunodeficiency virus transmission. Rational approaches to therapeutics in these conditions should benefit from understanding local pharmacokinetics and pharmacodynamics of active drugs within the male genital tract. However, the description of drug distribution into the male genital tract has been largely limited to total, rather than protein-free drug concentrations in the whole ejaculate at one or two time points within a dosing interval, which may be misleading in understanding local drug action. Recent innovations enable a quantitative understanding of protein-free drug kinetics into semen and drug distribution into individual male genital tract glands. These methods may benefit therapeutics through optimization of targeted drug delivery and facilitate drug development for diseases related to these glands.

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Section: Traditional Approaches To Study the Pharmacokinetics Of The mentioning

confidence: 99%

Male Genital Tract Pharmacology: Developments in Quantitative Methods to Better Understand a Complex Peripheral Compartment

Cao

2007

Clin Pharmacol Ther

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“…The first study on the concentration of antibiotics in ejaculate fluid was conducted by Armstrong et al (1968). These investigators examined whether unsuccessful treatment of prostatovesiculitis was due to inadequate tissue concentrations of 15 antimicrobial drugs.…”

Section: Results Of Early Studiesmentioning

confidence: 99%

“…The concentrations in the seminal plasma were similar to those in the total ejaculate. The median concen- Dalet et al (1978) 6.9 9.64 3.55 Armstrong et al (1968) 12.5 ± 2.3 ~g/gd Rubi & Galan (1979) 44.8 ± 14.9 ~g/gd 0.14 1. 16 Naberetal.…”

Section: Cephalosporinsmentioning

confidence: 99%

Drugs in Semen

Pichini

Zuccaro

Pacifici

1994

Clinical Pharmacokinetics

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Over the past 50 years, a decline in the quality of semen has been observed, possibly resulting in a reduction in male fertility. Among the factors affecting semen quality, exposure to drugs is of particular importance. It is known that drugs can be transported to the seminal plasma, which is made up of secretions from the various accessory genital glands. There is evidence that many drugs enter the male genitourinary tract by an ion-trapping process. Lipid solubility and the degree of ionisation of the drug, which depend on the pH of plasma and seminal fluid, are important factors in this process. To date, few studies have been conducted on this topic. Pharmacokinetic evaluation of the fluids of the male accessory gland have been performed in the case of chloroquine and caffeine only, while the effects of mesalazine (5-aminosalicylic acid), sulfasalazine, salicylate, propranolol, diltiazem, flunarizine, verapamil, caffeine and nicotine on sperm physiology and morphology have been examined. Although data from the literature are scarce and incomplete, it is evident that many drugs can be excreted into semen. These drugs may interfere with the most common semen characteristics, potentially resulting in a male-mediated teratogenic effect, or local and systemic responses in female recipients. Therefore, it may be advisable to include, in the processes of drug development, pharmacokinetic evaluation of a drug in the semen and analysis of standard microscopic parameters of the semen. This is particularly important for drugs known to concentrate in the semen.

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“…A survey of the literature, however, shows that only few antibiotics or other antibacterial drugs such as trimethoprim and sulfamethoxazole accumulate in the prostate and are thence excreted in the semen (Eliasson and Dornbusch 1977;Asher et al 1978). Of 15 different antibiotics tested by Armstrong (1968),…”

Section: Discussionmentioning

confidence: 99%

“…Cephalexin has been reported to accumulate in prostatic tissue (Symes et al 1974), and also to be secreted into the ejaculum (Symes et al 1974;Dalet et al 1978;Armstrong 1968). This probably accounts for the wide use of Cephalexin in inflammations of the urogenital tract (Stamey et al 1970).…”

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confidence: 99%

Absence in Human Ejaculate of Cephalexin Following its Oral Administration

et al. 1979

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Cephalexin (1 g) was ingested by 57 male volunteers and the subsequent concentrations of the drug in their serum and ejaculate were measured by the broth‐dilution method. Serum maximal levels (29.8 ± 6.6 μg/ml) were attained 1 h following ingestion and were sustained for an additional h before dropping to about 10% at 4 h postingestion. In the ejaculates, 22 out of 34 determinations failed to detect the drug whereas the remaining 12 gave various levels apparently independet of the time elapsed from drug administration. Determinations of the drug in the two fractions of 15 split ejaculates showed measurable levels in only 8 ejaculates and these were invariably higher in the first fraction than in the second. Cephalexin levels in the urine of 8 men 2 h after ingestion of the drug were above 200 μ/ml. Ejaculates obtained from these men half an h after the micturition showed in 7 out of 8 cases Cephalexin levels in the range of 12–50 μ/ml. These findings suggest that contamination of the ejaculate by traces of urine (from the urethra) may explain some false‐positive results reported in the literature for Cephalexin in seminal plasma.

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Concentration of Antibiotic and Chemotherapeutic Agents in the Ejaculum

Cited by 24 publications

References 7 publications

Male Genital Tract Pharmacology: Developments in Quantitative Methods to Better Understand a Complex Peripheral Compartment

Male Genital Tract Pharmacology: Developments in Quantitative Methods to Better Understand a Complex Peripheral Compartment

Drugs in Semen

Absence in Human Ejaculate of Cephalexin Following its Oral Administration

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